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((1E)-2-nitroprop-1-en-1-yl)benzene
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50% inhibition at 0.023 mM in absence of 2-mercaptoethanol, at 0.515 mM in presence of 1 mM 2-mercaptoethanol
((2-bromo-4-((((2E)-3-phenylprop-2-en-1-yl)sulfanyl)methyl)phenyl)carbonyl)phosphonate
50% inhibition at 810 nM for wild-type, at 1290 nM for mutant S295F
((2-bromo-4-(((4-chlorobenzyl)thio)methyl)phenyl)(difluoro)methyl)phosphonate
50% inhibition at 285 nM for wild-type, at 1644 nM for mutant S295F
((2-phenyl-2-(phenylcarbonyl)propane-1,3-diyl)bis(benzene-4,1-diyl(difluoromethanediyl)))bis(phosphonate)
50% inhibition at 82 nM for wild-type, at 399 nM for mutant S295F
((4-((((3'-(acetylsulfamoyl)biphenyl-4-yl)methyl)sulfanyl)methyl)-2-bromophenyl)(difluoro)methyl)phosphonate
50% inhibition at 2.2 nM for wild-type, at 11 nM for mutant S295F
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonate
50% inhibition at 47 nM for wild-type, at 260 nM for mutant S295F
((4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)phenyl)(fluoro)methyl)phosphonate
50% inhibition at 570 nM for wild-type, at 830 nM for mutant S295F
((4-((4E)-2-(1H-benzotriazol-1-yl)-2,5-diphenylpent-4-en-1-yl)phenyl)(difluoro)methyl)phosphonic acid
-
50% inhibition at 109 nM for isoform PTP-1B, at 95 nM for isoform TCPTP
((E)-2-nitrovinyl)benzene
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i.e. trans-beta-nitrostyrene, slow-binding inhibitor, acting as a pY mimetic and binding to the enzyme active site to form an initial noncovalent E*I complex, followed by nucleophilic attack on the nitrostyrene nitro group by C215 of enzyme to form a reversible, covalent adduct. 50% inhibition at 0.0025 mM in absence of 2-mercaptoethanol, at 0.4 mM in presence of 1 mM 2-mercaptoethanol
(1-benzyl-3-methyl-2,3-dihydro-1H-imidazol-2-yl)(chloro)gold
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i.e. [(BzMeIm)AuICl]
(1R,3aS,3bS,10aR,10bS,12aR)-1-[(2R)-4-carboxybutan-2-yl]-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,7,10,10a,10b,11,12,12a-tetradecahydrocyclopenta[5,6]naphtho[1,2-f]indazole-9-carboxylic acid
-
-
(1R,5S,6S,6aR,7S,10S,10aS,11S)-10-(acetyloxy)-7-hydroxy-7,10a-dimethyl-4-methylidene-6-[(2-methylpropanoyl)oxy]-3-oxodecahydro-1H-1,5-methano-2-benzoxocin-11-yl 2-methylprop-2-enoate
no inhibition at 0.021 mM
(1S,3aR,8S,8aS,8bR)-4-henicosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,5a,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione
-
-
(1S,3aS,4R,8S,8aS,8bR)-4-icosyl-1,8-dimethyl-3a-[(1E)-tricos-1-en-1-yl]-1,3a,4,8,8a,8b-hexahydrobenzo[1,2-c:3,4-c']difuran-3,6-dione
-
-
(2alpha,3alpha)-2,3-dihydroxyolean-12-en-28-oic acid
-
-
(2aS,3R,6aR,7aS,7bR,7cS)-2a-(hydroxymethyl)-3-icosyl-6a,7a-dimethyl-2a,3,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2,5-dione
-
-
(2aS,3R,6aR,7aS,7bR,7cS)-3-icosyl-6a,7a-dimethyl-2,5-dioxo-3,5,6a,7a,7b,7c-hexahydrodifuro[2,3,4-cd:4',3',2'-hi][2]benzofuran-2a(2H)-carbaldehyde
-
-
(2beta,3beta)-2,3-dihydroxyolean-12-en-28-oic acid
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(2E)-1-(2'-hydroxyphenyl)-3-(1-naphthyl)-2-propen-1-one
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76% inhibition at 0.025 mM
(2E)-1-(2,4-dihydroxyphenyl)-3-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-1-(2,4-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
20% inhibition at 0.025 mM
(2E)-1-(2,4-dimethoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
-
(2E)-1-(2,5-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one
-
58% inhibition at 0.025 mM
(2E)-1-(2,5-dimethoxyphenyl)-3-(naphth-1-yl)-2-propen-1-one
-
46% inhibition at 0.025 mM
(2E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
-
8% inhibition at 0.025 mM
(2E)-1-(2-hydroxy-4,6-dimethoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
16% inhibition at 0.025 mM
(2E)-1-(2-hydroxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
26% inhibition at 0.025 mM
(2E)-1-(3,4-dimethoxyphenyl)-3-(2-naphthyl)-2-propen-1-one
-
-
(2E)-1-(3,4-dimethoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
68.5% inhibition at 0.025 mM
(2E)-1-(3-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(3-hydroxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
20% inhibition at 0.025 mM
(2E)-1-(3-methoxy-4-hydroxyphenyl)-3-(2-naphthyl)-2-propen-1-one
-
-
(2E)-1-(3-methoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
18.5% inhibition at 0.025 mM
(2E)-1-(4-aminophenyl)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-1-(4-bromophenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
-
25% inhibition at 0.025 mM
(2E)-1-(4-bromophenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
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11% inhibition at 0.025 mM
(2E)-1-(4-hydroxy-3-methoxyphenyl)-3-(naphthalen-2-yl)prop-2-en-1-one
-
39% inhibition at 0.025 mM
(2E)-1-(4-methoxyphenyl)-3-(naphthalen-1-yl)prop-2-en-1-one
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18% inhibition at 0.025 mM
(2E)-1-[3-(benzyloxy)phenyl]-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-2-[1-carbamothioyl-3-(4-nitrophenyl)-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]-1-(4-sulfophenyl)diazanide
-
-
(2E)-2-[[5-(3-carboxy-4-hydroxycyclohexa-1,5-dien-1-yl)furan-2-yl]methylidene]-1-[6-[(4-fluorophenyl)amino][1,2,5]oxadiazolo[3,4-b]pyrazin-5-yl]diazanide
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
-
8% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2,5-dimethoxyphenyl)prop-2-en-1-one
-
9% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
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-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
18% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(3,4-dimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(3-nitrophenyl)prop-2-en-1-one
-
26% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
-
14% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-hydroxy-3-methoxyphenyl)prop-2-en-1-one
-
20% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-methoxyphenyl)prop-2-en-1-one
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6% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-nitrophenyl)prop-2-en-1-one
-
19.5% inhibition at 0.025 mM
(2E)-3-(1,3-benzodioxol-5-yl)-1-phenylprop-2-en-1-one
-
-
(2E)-3-(3,4-dichlorophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(3-chlorophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(3-chlorophenyl)-1-(2-hydroxy-4,6-dimethoxyphenyl)prop-2-en-1-one
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13% inhibition at 0.025 mM
(2E)-3-(3-nitrophenyl)-1-(2,4,6-trimethoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-(5-bromo-2,4-dihydroxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(3-[[(methoxycarbonyl)sulfanyl]amino]phenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-butoxyphenyl)prop-2-en-1-one
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-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-hydroxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-(4-methoxyphenyl)prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-(piperidin-1-yl)phenyl]prop-2-en-1-one
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-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[2-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(3-methylbut-3-en-2-yl)-4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
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-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-(piperidin-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[3-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(1H-pyrazol-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(dimethylamino)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(methylsulfonyl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(morpholin-4-yl)phenyl]prop-2-en-1-one
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-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-(piperidin-1-yl)phenyl]prop-2-en-1-one
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-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
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-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-hydroxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-methoxy-3-(prop-2-en-1-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(3-methylbut-2-en-1-yl)oxy]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[(4-methylphenyl)sulfonyl]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[4-[di(prop-2-en-1-yl)amino]phenyl]prop-2-en-1-one
-
-
(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)-1-[6-(dimethylamino)-1,3-benzodioxol-5-yl]prop-2-en-1-one
-
-
(2E)-3-(naphthalen-1-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
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(2E)-3-(naphthalen-1-yl)-1-(3-nitrophenyl)prop-2-en-1-one
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12% inhibition at 0.025 mM
(2E)-3-(naphthalen-1-yl)-1-(4-nitrophenyl)prop-2-en-1-one
-
18% inhibition at 0.025 mM
(2E)-3-(naphthalen-1-yl)-1-phenylprop-2-en-1-one
-
37% inhibition at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
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9% activation at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-(3-nitrophenyl)prop-2-en-1-one
-
16% inhibition at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-(4-nitrophenyl)prop-2-en-1-one
-
11% inhibition at 0.025 mM
(2E)-3-(naphthalen-2-yl)-1-phenylprop-2-en-1-one
-
12% inhibition at 0.025 mM
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[4-hydroxy-2-methoxy-3-(3-methylbut-2-en-1-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]-1-(4-methoxyphenyl)prop-2-en-1-one
-
a semisynthetic licochalcone A derivative
(2E)-3-[4-hydroxy-2-methoxy-5-(3-methylbut-3-en-2-yl)phenyl]-1-(4-hydroxyphenyl)prop-2-en-1-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
(2E)-3-[5-bromo-2-hydroxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-methoxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2E)-3-[5-bromo-2-methoxy-4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-1-[4-hydroxy-3-(3-methylbut-3-en-2-yl)phenyl]prop-2-en-1-one
-
-
(2R)-2-benzyl-3-[2,6-dibromo-4-(6-bromo-5a,11a-dihydrobenzo[b]naphtho[2,3-d]furan-11-yl)phenyl]propanoic acid
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(2Z)-2-([5-[4-(1H-tetrazol-1-yl)phenyl]furan-2-yl]methylidene)[1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
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(2Z)-2-[[5-(2-methyl-5-nitrophenyl)furan-2-yl]methylidene][1,3]thiazolo[3,2-a]benzimidazol-3(2H)-one
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(3alpha,5beta,8alpha,9beta,10alpha,13alpha)-3-[[(2E)-4-phenylbut-2-enoyl]oxy]kaur-16-en-18-oic acid
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(3aR,4R,4aR,5R,8R,8aR,9S,9aR)-8-(acetyloxy)-5-hydroxy-5,8a-dimethyl-3-methylidene-4-[(2-methylpropanoyl)oxy]-2-oxododecahydronaphtho[2,3-b]furan-9-yl 3-methylbutanoate
no inhibition at 0.020 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylprop-2-enoate
no inhibition at 0.025 mM
(3aR,4R,4aR,5R,8R,8aS,9S,9aR)-8-(acetyloxy)-5,9-dihydroxy-5,8a-dimethyl-3-methylidene-2-oxododecahydronaphtho[2,3-b]furan-4-yl 2-methylpropanoate
no inhibition at 0.024 mM
(3beta)-3-(acetyloxy)olean-12-en-28-oic acid
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-
(3beta)-3-hydroxyolean-12-en-28-oic acid
-
-
(3beta)-3-hydroxyoleana-11,13(18)-dien-28-oic acid
-
-
(3S,3aR,4S,5R,7aR)-4-acetyl-7-henicosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,5,7a-hexahydro-2-benzofuran-5-carboxylic acid
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-
(3S,3aR,4S,7R,7aS)-4-acetyl-7-icosyl-3-methyl-1-oxo-7a-[(1E)-tricos-1-en-1-yl]-1,3,3a,4,7,7a-hexahydro-2-benzofuran-5-carboxylic acid
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-
(3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
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-
(3S,6S,9R,12R)-3,6,9-trimethyl-12-[(R)-phenyl(phenylamino)methyl]-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
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-
(3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(3Z)-5-bromo-3-[4-oxo-2-thioxo-3-[3-(trifluoromethyl)phenyl]-1,3-thiazolidin-5-ylidene]-1,3-dihydro-2H-indol-2-one
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-
(4-((4E)-2-(1,3-benzothiazol-2-yl)-2-(1H-benzotriazol-1-yl)-5-phenylpent-4-en-1-yl)benzyl)phosphonate
50% inhibition at 3260 nM for wild-type, at 5030 nM for mutant S295F
(4-fluorophenyl)[[(Z)-(2,2,2-trifluoro-1-[1-(4-fluorophenyl)-2-methyl-5-[4-(methylsulfonyl)phenyl]-1H-pyrrol-3-yl]ethylidene)amino]oxy]methanone
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-
(4-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-methoxy-3-oxopropyl]phenyl)methaneseleninic acid
-
inactivates the PTPs, e.g. YopH, by covalent modification, binds at the active site Cys403, kinetics, overview
(4aR,6aR,6bS,8aR,12aS,14aR,14bR)-8a-hydroxy-4,4,6a,6b,11,11,14b-heptamethyl-1,4a,5,6,6a,6b,7,8a,9,10,11,12,12a,14,14a,14b-hexadecahydropicene-3,8(2H,4H)-dione
-
-
(4aR,6aS,6bR,8aR,10S,12aR,12bR,14bS)-4a,10-dihydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-octadecahydropicen-5(1H)-one
-
-
(4aS,6aS,6bR,13aR)-10-acetyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
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-
(4aS,6aS,6bR,13aR)-10-hexanoyl-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-11-amino-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[3,2-d][1,3]thiazole-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,13,13a,13b,14,15b-hexadecahydropiceno[2,3-d][1,2]oxazole-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-3-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-(pyridin-4-ylcarbonyl)-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,13aR)-2,2,6a,6b,9,9,13a-heptamethyl-10-phenyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,13,13a,13b,14,15b-octadecahydro-4aH-chryseno[1,2-f]indazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-11-amino-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,11,14a-octamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinoxaline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-11-(methylamino)-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,15aR)-2,2,6a,6b,9,9,15a-heptamethyl-1,2,3,4,5,6,6a,6b,7,8,8a,9,10,15,15a,15b,16,17b-octadecahydro-4aH-chryseno[2,1-b]carbazole-4a-carboxylic acid
-
-
(4aS,6aS,6bR,16aR)-2,2,6a,6b,9,9,16a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,16,16a,16b,17,18b-hexadecahydrochryseno[1,2-b]phenazine-4a(2H)-carboxylic acid
-
-
(4E)-2-(3,4-dichlorophenyl)-4-(3,4,5-trimethoxybenzylidene)-1,3-oxazol-5(4H)-one
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,2,3]thiadiazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,6a,9a,10,10a,10b,11,12,12a-tetradecahydro-1H-cyclopenta[7,8]phenanthro[3,2-d][1,2]oxazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-7-phenyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoic acid
-
competitive PTP1B inhibitor
(4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,8,11a,13a-pentamethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoic acid
-
-
(5beta,8alpha,9beta,10alpha,13alpha)-kaur-16-en-18-oic acid
-
(5R)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5S)-2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
(5Z)-3-benzyl-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-benzyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-3-butyl-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-2,4-dimethoxybenzylidene)-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-butoxy-2-methoxybenzylidene)-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-(5-bromo-4-hydroxy-2-methoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[2-methoxy-5-(prop-2-en-1-yl)-4-(tetrahydro-2H-pyran-2-yloxy)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-(benzyloxy)-5-bromo-2-methoxybenzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(3-methylbut-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(prop-2-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-(propan-2-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[4-hydroxy-2-methoxy-5-(prop-2-en-1-yl)benzylidene]-3-methyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(prop-2-en-1-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-(propan-2-yloxy)benzylidene]-3-butyl-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(3-methylbut-2-en-1-yl)oxy]benzylidene]-1,3-thiazolidine-2,4-dione
-
(5Z)-5-[5-bromo-2-methoxy-4-[(4-methylpent-3-en-1-yl)oxy]benzylidene]-3-(4-methylpent-3-en-1-yl)-1,3-thiazolidine-2,4-dione
-
(6aS,6bR,8aR,10S,12aS,12bR)-10-hydroxy-2,2,6a,6b,9,9,12a-heptamethyl-2,3,4,4a,6,6a,6b,7,8,8a,9,10,11,12,12a,12b-hexadecahydropicen-5(1H)-one
-
-
(6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione
-
-
(7bS,9R,13bR,15R)-7-amino-9-(hydroxymethyl)-10,13-dioxo-2,3,3a,3b,4,5,6,7,7a,7b,9,10,13,13b-tetradecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-15-carbonitrile
inhibits Cdc25B modestly
(7bS,9R,13bR,15S)-7-amino-15-hydroxy-9-(hydroxymethyl)-2,3,3a,3b,4,5,6,7,7a,7b,9,13b-dodecahydro-1H-6,8-methanobenzo[h]imidazo[1,2-a]pyrido[3,2-c][1,5]naphthyridine-10,13-dione
-
(9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
-
(difluoro(4-((4E)-2-((4-fluorophenyl)carbonyl)-2-(4-(3-methyl-1,2,4-oxadiazol-5-yl)phenyl)-5-phenylpent-4-en-1-yl)phenyl)methyl)phosphonic acid
-
50% inhibition at 163 nM for PTP-1B wild-type, at 1903 nM for PTP-1B mutant L119V, and at 1600 nM for isoform TCPTP wild-type and 138 nM for TCPTP mutant V121L
(difluoro[4-[(2,2,2-trifluoroethyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(2-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(2-phenylethyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(3-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(4-fluorophenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[(phenylamino)methyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[2-oxo-2-(phenylamino)ethyl]phenyl]methyl)phosphonic acid
-
(difluoro[4-[methyl(phenyl)carbamoyl]phenyl]methyl)phosphonic acid
-
(E)-N-(4,5-diphenyl-1,3-thiazol-2-yl)-2-naphthalen-2-ylethenesulfonamide
-
(E)-N-[4-(4-chlorophenyl)-5-propyl-1,3-thiazol-2-yl]-2-(3,4-dichlorophenyl)ethenesulfonamide
-
(Z)-1-(3-(3-carboxy-3-hydroxyacryloyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 2.4 mg/ml
(Z)-1-(3-(4-ethoxy-3-hydroxy-4-oxobut-2-enoyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 3.1 mg/ml
(Z)-2-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(2-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
-
-
(Z)-3-(2-(2-nitrophenyl)hydrazono)-2-oxoindoline-5-sulfonic acid
-
NSC-117199
(Z)-3-(2-(3-carboxyphenyl)hydrazono)-2-oxoindoline-5-carboxylic acid
-
-
(Z)-3-(2-(5-(4-chlorobenzylcarbamoyl)-2-oxoindolin-3-ylidene)-hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(2,4-dichlorophenethyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(3-chloro-4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(3-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-3-(2-(5-(N-(4-methylbenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(2-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-chloro-3-(trifluoromethyl)benzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-chlorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-(4-fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid
-
-
(Z)-4-(2-(5-(N-benzylsulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl) benzoic acid
-
-
([2-bromo-4-(3-oxo-2,3-diphenylpropyl)phenyl](difluoro)methyl)phosphonic acid
-
1,1'-(piperazine-1,4-diyl)bis(4-(3-(dibenzylamino)phenyl)butane-1,2,4-trione)
-
-
1,2-Cyclohexanedione
-
40% inhibition at 1 mM
1,3-difluoro-2-[(E)-2-nitroethenyl]benzene
-
50% inhibition at 0.0048 mM in absence of 2-mercaptoethanol, at 0.34 mM in presence of 1 mM 2-mercaptoethanol
1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
15.1% inhibition at 0.02 mg/ml
1,6-dimethyl-3-(thiophen-2-yl)pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
-
1-(1,3-benzodioxol-5-yl)-2-([1-(4-hydroxyphenyl)-1H-1,2,3,4-tetraazol-5-yl]sulfanyl)-1-ethanone
88% inhibition at 0.2 mM
1-(2,6-dihydroxy-4-methoxy-3-methylphenyl)ethanone
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
36.2% inhibition at 0.02 mg/ml
1-(4-hydroxy-3-(methoxycarbonyl)benzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 8.1 mg/ml
1-benzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
15.1% inhibition at 0.02 mg/ml
1-benzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
3.1% inhibition at 0.02 mg/ml
1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
0.7% inhibition at 0.02 mg/ml
1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
0.8% inhibition at 0.02 mg/ml
1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
3.5% inhibition at 0.02 mg/ml
1-cyclopropyl-N-(4-fluorobenzyl)-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
3.3% inhibition at 0.02 mg/ml
1-ethyl-3-dimethylaminopropyl carbodiimide
-
90% inhibition at 25 mM
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
1-methoxy-4-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.0045 mM in absence of 2-mercaptoethanol, at 0.27 mM in presence of 1 mM 2-mercaptoethanol
1-methyl-4-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.003 mM in absence of 2-mercaptoethanol, at 0.225 mM in presence of 1 mM 2-mercaptoethanol
1-p-Bromotetramisole oxalate
-
tetramizole no effect
1-[(5Z)-5-(1-butyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene)-4-oxo-4,5-dihydro-1,3-thiazol-2-yl]piperidine-4-carboxamide
-
-
1-[4-[(2-nitrophenyl)sulfonyl]piperazin-1-yl]-2-phenoxyethanone
-
-
15-hydroxykaur-9(11),16-dien-19-oic acid
-
16alphaH,17-isovaleryloxy-ent-kauran-19-oic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.007 mM, noncompetitive
19alpha,24-dihydroxyurs-12-en-3-on-28-oic acid
-
-
2',4'-dihydroxy-1,1'-biphenyl
-
2,2'-[benzene-1,4-diylbis(methanediyloxybenzene-4,1-diyl)]bis(oxoacetic acid)
-
-
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
2,4-dihydroxy-6-methylbenzoic acid
-
45% inhibition of PTPB1 at 0.178 mM
2,4-dimethoxy-1-((E)-2-nitrovinyl)benzene
-
50% inhibition at 0.028 mM in absence of 2-mercaptoethanol, at 0.390 mM in presence of 1 mM 2-mercaptoethanol
2,5-dihydroxy-3-[7-(2-methylbenzyl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
-
2,5-dihydroxy-3-[7-(3-methylbut-2-en-1-yl)-1H-indol-3-yl]cyclohexa-2,5-diene-1,4-dione
-
2-((carboxycarbonyl)amino)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
i.e. OATP
2-((carboxycarbonyl)amino)-5-((1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-fluoro-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((4-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-((carboxycarbonyl)amino)-5-((5-hydroxy-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl)-4,7-dihydro-5H-thieno(2,3-c)pyran-3-carboxylic acid
-
2-(2,5-dimethyl-1H-pyrrol-1-yl)-5-hydroxybenzoic acid
-
36% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 7% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
2-(4-hydroxyphenyl)-3-[(3,4-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
2-(4-hydroxyphenyl)-3-[(4-carboxy-3-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
2-(oxalyl-amino)-4,5,6,7-tetrahydro-thieno[2,3-c]pyridine-3-carboxylic acid
-
2-(oxalyl-amino)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid
-
2-(oxalyl-amino)-4,7-dihydro-5H-thieno[2,3-c]thiopyran-3-carboxylic acid
-
-
2-carboperoxybenzoate
-
complete inhibition at 150 mM
2-chloro-4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
36% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 95% residual activity at 0.1 mM; 98% residual activity at 0.1 mM
2-chloro-5-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
37% residual activity at 0.1 mM; 77% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 91% residual activity at 0.1 mM
2-hydroperoxytetrahydrofuran
-
inactivation by 2-hydroperoxytetrahydrofuran (0.05 mM, 10 min) is reversed upon reaction of the enzyme with dithiothreitol (54% return of activity, following treatment with 100 mM dthiothreitol for 1 h)
2-[(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)imino]-1H-indene-1,3(2H)-dione
-
-
2-[(carboxycarbonyl)amino]-4,5,6,7-tetrahydro-thieno[2,3-c]-pyridine-3-carboxylic acid
i.e. TCS401, binds to the active site
2-[4,5-bis(1,3,2-dithiarsolan-2-yl)-6-hydroxy-3-oxo-3H-xanthen-9-yl]benzoic acid
i.e. FlAsH
2-[6-chloro-5-(1-naphthalyloxy)-1H-benzimidazol-2-yl]thio-N-(thiazol-2-yl)acetamide
mixed-type inhibition, 99% inhibition at 0.2 mM
24-hydroxyursolic acid
-
-
28-(10-decanoic)-oleanolic acid
-
28-(12-dodecanoic)-oleanolic acid
-
28-(2-acetic)-oleanolic acid
-
28-(4-butyric)-oleanolic acid
-
28-(6-hexanoic)-oleanolic acid
-
28-(8-octanoic)-oleanolic acid
-
28-(glycine)-oleanolic acid amide
-
28-(L-glutamic acid)-oleanolic acid amide
-
28-(L-phenylalanine)-oleanolic acid amide
-
28-(p-carboxyphenyl)-oleanolic acid amide
-
28-[4-butyric((R)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-3-indole-ethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-5-imidazole-ethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-methylthioethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric((S)-1-carboxy-phenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-2,3-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,4-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,4-oxymethyleneoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-3,5-dimethoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-m-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-m-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-o-methylphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-chlorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-fluorophenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-methoxyphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-methylphenylethyl)-amide]-DELTA12-oleanene
-
28-[4-butyric(1-carboxy-p-nitrophenylethyl)-amide]-DELTA12-oleanene
-
2alpha,3alpha,19alpha,23-tetrahydroxyurs-12-en-28-oic acid
-
50% inhibition at 0.0421 mM
2beta,3beta-2,3-dihydroxyolean-12-en-28-oic acid
-
-
3',4'-dihydroxy-1,1'-biphenyl
no inhibition of LMW-PTP isozymes, but 5% inhibition of PTP-B1 at 0.02 mM
3,16-dioxo-olean-12(13),17(18)-diene
-
-
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-(1,3-thiazol-2-ylsulfamoyl)phenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.008 mM, noncompetitive noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-((3,5-dibromo-4-hydroxyphenyl)carbonyl)-2-ethyl-N-(4-sulfamoylphenyl)-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.022 mM, noncompetitive allosteric inhibitor, prevents formation of the active form of the enzyme by blocking the mobility of the catalytic loop
3-(1-carboxy-ethoxy)-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-(2,2'-dimethyl-carboxypropanoyloxy)-oleanolic acid
-
3-(2,5-dimethyl-1H-pyrrol-1-yl)-4-hydroxybenzoic acid
-
20% residual activity at 0.1 mM; 3% residual activity at 0.1 mM; 52% residual activity at 0.1 mM; 7% residual activity at 0.1 mM
3-(2-carboxy-benzyloxy)-oleanolic acid
-
3-(2-carboxybenzoyloxy)-oleanolic acid
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide
50% inhibition of PTP1B at 0.35 mM
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N-[4-(1,3-thiazol-2-ylsulfamoyl)phenyl]-1-benzofuran-6-sulfonamide
-
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-(4-(thiazol-2-yl-sulfamyl)-phenyl)-amide
-
a PTP1b inhibitor, inhibit 50% tog the infectivity of Trypanosoma cruzi trypomastigotes
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethylbenzofuran-6-sulfonic acid-[4-(thiazol-2-ylsulfamyl)phenyl]-amide
i.e. BBR
3-(3-carboxy-benzyloxy)-oleanolic acid
-
3-(4-carboxy-benzyloxy)-28-[4-butyric((s)-1-carboxyphenylethyl)-amide]-DELTA12-oleanene
-
3-(4-carboxy-benzyloxy)-oleanolic acid
-
3-(4-chlorophenyl)-1,6-dimethylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
-
3-(biphenyl-4-ylmethyl)-6-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
-
3-(carboxy-fluoro-methoxy)-6-chloro-benzo(b)thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-2-naphthoic acid
-
-
3-(carboxymethoxy)-5-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-5-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-5-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-((1-(ethylsulfonyl)-piperidin-4-yl)amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-((cyclohexylmethyl)-amino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-(cyclohexylamino)-thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-(tetrahydro-2H-pyran-4-ylamino)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-chlorothieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)-6-methylthieno(3,2-c)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)benzo(b)thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)furo(2,3-b)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(2,3-b)pyridine-2-carboxylic acid
-
reversible, competitive
3-(carboxymethoxy)thieno(3,2-b)(1)benzo-thiophene-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(3,2-b)pyridine-2-carboxylic acid
-
-
3-(carboxymethoxy)thieno(3,2-b)thiophene-2-carboxylic acid
-
-
3-([2-chloro-6-methoxy-4-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]phenoxy]methyl)benzoic acid
-
3-benzyl-7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
3-benzyloxy-oleanolic acid
-
3-butyl-7-(2,4-dihydroxy-6-pentylphenoxy)-3,5-dimethoxy-2-benzofuran-1(3H)-one
-
a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-carboxymethoxy-6-(4-hydroxyphenyl)-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-(5-methyl-1-phenyl-1H-pyrazol-3-ylcarbamoyl)-benzo(b)thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-phenylbenzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-6-thiophen-2-yl-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-7-chloro-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-7-methyl-benzo(b)-thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-naphtho(1,2-b)thiophene-2-carboxylic acid
-
-
3-carboxymethoxy-thieno(3,2-c)quinoline-2-carboxylic acid
-
-
3-carboxypropanoyloxy-oleanolic acid
-
3-chlorobenzenecarboperoxoic acid
-
complete inhibition at 150 mM
3-dehydroxy-oleanolic acid
-
3-ethyl oxalyl-oleanolic acid
-
3-hydroxy-4-(methoxycarbonyl)-2,5-dimethylphenyl 3-acetyl-2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-hydroxy-4-(methoxycarbonyl)-5-methylphenyl 4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoate
-
-
3-methyl-2-butenal
-
95% remaining activity at 0.5 mM
3-methylene-oleanolic acid
-
3-oxalyl-oleanolic acid
-
3-[(1-butyl-1,6-dimethoxy-3-oxo-1,3-dihydro-2-benzofuran-4-yl)oxy]-4,6-dihydroxy-2-pentylbenzoic acid
-
a pseudodepsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonamide
-
-
3-[(2-nitrophenyl)hydrazono]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid 4-chlorobenzylamide
-
-
3-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
3-[(E)-(3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]benzoic acid
-
3-[2,5-dimethyl-3-[(3-oxo-2,3-dihydro[1,3]thiazolo[3,2-a]benzimidazol-2-yl)methyl]-1H-pyrrol-1-yl]benzoic acid
irreversible inhibition, detailed kinetic analysis of the interaction between E4 and the catalytic domain of enzyme STEP, overview. kinact is 0.068/s
3-[3-(2,4-dichlorophenyl)propanoyl]-2-hydroxycyclohepta-2,4,6-trien-1-one
-
3-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
-
-
3-[oxalyl-amino]naphthalene-2-carboxylic acid
-
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,6-dicarboxylic acid
-
25% residual activity at 0.1 mM; 39% residual activity at 0.1 mM; 65% residual activity at 0.1 mM; 73% residual activity at 0.1 mM
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4,8-dicarboxylic acid
-
30% residual activity at 0.1 mM; 53% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 79% residual activity at 0.1 mM
3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
23% residual activity at 0.1 mM; 75% residual activity at 0.1 mM; 80% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
3alpha-angeloyloxypterokaurene L3
18% inhibition at 0.024 mM
3alpha-cinnamoyloxypterokaurene L3
-
3alpha-tigloyloxypterokaurene L3
no inhibition at 0.024 mM
3beta,16a,17-trihydroxy-olean-12-ene
-
-
3beta-acetoxy-17beta-hydroxy-28-norolean-12-ene
-
-
3beta-acetoxy-28-hydroxyolean-12-ene
-
-
3beta-acetoxyolean-12-en-28-acid
-
-
3beta-acetoxyolean-12-en-28-aldehyde
-
-
3beta-hydroxyolean-12-en-28-oic acid
-
-
4'-carboxy-3'-hydroxy-1,1'-biphenyl
no inhibition of LMW-PTP isozymes, but 10% inhibition of PTP-B1 at 0.02 mM
4'-[(2-butyl-1-benzofuran-3-yl)methyl]biphenyl-4-ol
-
4'-[2-(4-hydroxybutyl)-1-benzofuran-3-yl]biphenyl-4-ol
-
4,4'-[benzene-1,4-diylbis(methanediyloxy)]dibenzoic acid
-
4,6-bis(1,3,2-dithiarsolan-2-yl)-7-hydroxy-3H-phenoxazin-3-one
i.e. ReAsH
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenoxyphenyl)methylidene]thiazolidin-3-yl) methyl)benzoic acid
-
4-(((5Z)-2-(4-fluorophenylimino)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]thiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(3-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-(((5Z)-4-oxo-5-[(4-phenylmethoxyphenyl)methylidene]-2-thioxothiazolidin-3-yl)methyl)benzoic acid
-
4-((3E)-1-(1H-benzotriazol-1-yl)-1-(4-(difluoro(phosphono)methyl)benzyl)-4-phenylbut-3-en-1-yl)benzoic acid
-
50% inhibition at 39 nM for wild-type PTP-1B, at 39 nM for mutant V113I, at 45 nM for mutant M114V, at 29 nM for mutant V113I/M114V, at 32 nM for mutant G117E, at 142 nM for mutant L119V, and at 87 nM for isoform TCPTP wild-type and 24 nM for isoform TCPTP mutant V121L
4-((E)-2-nitrovinyl)benzoic acid
-
50% inhibition at 0.0027 mM in absence of 2-mercaptoethanol, at 0.425 mM in presence of 1 mM 2-mercaptoethanol
4-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
63% residual activity at 0.1 mM; 6% residual activity at 0.1 mM; 88% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
4-(2,5-dimethyl-1H-pyrrol-1-yl)-3-hydroxybenzoic acid
-
21% residual activity at 0.1 mM; 67% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 9% residual activity at 0.1 mM
4-(2,5-dimethyl-1H-pyrrol-1-yl)phthalic acid
-
18% residual activity at 0.1 mM; 54% residual activity at 0.1 mM; 78% residual activity at 0.1 mM; 80% residual activity at 0.1 mM
4-(3-(dibenzylamino)phenyl)-2,4-dioxobutanoic acid
-
-
4-(5-bromo-1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)-2-hydroxybenzoic acid
-
4-(5-[5-(3,5-dichlorophenoxy)-2-furyl]-1,2,4-oxadiazol-3-yl)phenyl-N,N-dimethylsulfamate
85% inhibition at 0.2 mM
4-(beta-D-galactopyranosyloxy)-2-hydroxy-6-pentadecylbenzoic acid
-
-
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
4-(difluoro(phosphono)methyl)-N-pentadecanoyl-L-phenylalanyl-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
dose-dependent increase in Y527 phosphorylation of Src
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-methoxyphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2-[(4-tert-butylphenyl)imino]-4-oxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5E)-5-[3-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(3-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2,4-dioxo-5-[(4-phenoxyphenyl)methylidene]-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([3-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-2-(4-fluorophenylimino)-4-oxo-5-([4-(2-phenylethoxy)phenyl]methylidene)thiazolidin-3-yl]methyl)benzoic acid
-
4-([(5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene)-2-thioxothiazolidin-3-yl]methyl]benzoic acid
-
4-([(5Z)-5-[4-(benzyloxy)benzylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl)benzoic acid
-
4-chloro-N-(6-ethoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-chloro-N-(6-methoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-chloro-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-chloro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-fluoro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-fluorobenzyl-1-cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
73% inhibition at 0.02 mg/ml
4-hydroxymercuribenzoate
-
62% inhibition at 2.5 mM
4-isoavenaciolide
potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-(4-methoxyphenyl)isoxazole
-
4-methoxy-3-(5-methoxy-1-benzofuran-6-yl)-5-phenylisoxazole
-
4-methoxy-N-(6-methoxy-1,3-benzothiazol -2-yl)benzenesulfonamide
-
-
4-methoxy-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-methoxy-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-methyl-N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-methyl-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-nitro-N-(6-nitro-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
4-nitrocatechol sulfate
-
applied from from bare and amine functionalized mesoporous silica, MCM-48, and mesoporous alumina for sustained delivery, competitive inhibition, kinetics, overview
4-nitrophenyl phosphate
substrate inhibition at higher concentrations; substrate inhibition at higher concentrations
4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.073 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6,8-diphenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.0033 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0062 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-6-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.014 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-oxo-8-(phenylsulfanyl)-1,4-dihydro-1,7-naphthyridine-3-carboxylic acid
-
4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
4-[(1E)-3-(4-hydroxyphenyl)-3-oxoprop-1-en-1-yl]-5-methoxy-2-(2-methylbut-3-en-2-yl)phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2,4-dihydroxy-6-pentadecylbenzoyl)oxy]-2-hydroxy-6-methylbenzoic acid
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-bromobenzoate
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl 4-tert-butylbenzoate
-
-
4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl benzoate
-
-
4-[(2E)-3-[2,4-dimethoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2E)-3-[4-(acetyloxy)-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(2E)-3-[4-hydroxy-2-methoxy-5-(2-methylbut-3-en-2-yl)phenyl]prop-2-enoyl]phenyl acetate
-
a semisynthetic licochalcone A derivative
4-[(3-[(E)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(3-[(E)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[(2Z)-3-(4-carboxybenzyl)-4-oxo-2-(phenylimino)-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[(4-[(Z)-[3-(4-carboxybenzyl)-2,4-dioxo-1,3-thiazolidin-5-ylidene]methyl]phenoxy)methyl]benzoic acid
-
4-[1,3-dioxo-5-(4-oxo-4H-3,1-benzoxazin-2-yl)-1,3-dihydro-2H-isoindol-2-yl]benzoate
-
-
4-[2-[(5-chloro-1,3-benzoxazol-2-yl)sulfanyl]acetamido]benzoic acid
-
4-[4,5-di(biphenyl-4-yl)-1H-imidazol-2-yl]benzoic acid
-
-
4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoic acid
-
-
4-[difluoro(phosphono)methyl]benzoic acid
-
4-[N'-(5-isopropylsulfamoyl-2-oxo-1,2-dihydroindol-3-ylidene)-hydrazino]benzoic acid
-
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-methoxyphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-2-[(4-tert-butylphenyl)imino]-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(3-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[(4-phenoxyphenyl)methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-4-oxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2E,5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5E)-5-[3-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(2Z,5Z)-5-[4-(benzyloxy)benzylidene]-4-oxo-2-(phenylimino)-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5E)-5-(3-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[3-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-2,4-dioxo-5-[[4-(2-phenylethoxy)phenyl]methylidene]-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-(4-[[4-(hydroxymethyl)benzyl]oxy]benzylidene)-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[3-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
4-[[(5Z)-5-[[4-(benzyloxy)phenyl]methylidene]-2,4-dioxo-1,3-thiazolidin-3-yl]methyl]benzoic acid
-
5,7-bis[(E)-2-[4-(dimethylamino)phenyl]ethenyl]-2-methyltetrazolo[1,5-a]pyrimidin-2-ium
-
-
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E)-3-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]prop-1-en-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy3, 70% inhibition at 250 nM AsCy3, AsCy3 is capable of specifically and potently inhibiting mutant enzyme asPTP1B in the presence of a complex proteome, while AsCy3 does not inhibit wild-type PTP1B activity in a cell lysate
5-(1,3,2-dithiarsolan-2-yl)-2-[(1E,3E,5E)-5-[5-(1,3,2-dithiarsolan-2-yl)-3,3-dimethyl-1-(4-sulfobutyl)-1,3-dihydro-2H-indol-2-ylidene]penta-1,3-dien-1-yl]-3,3-dimethyl-1-(4-sulfobutyl)-3H-indol-1-ium
i.e. AsCy5
5-(2-fluoro-5-((1E)-3-[3-hydroxy-2-(methoxycarbonyl)phenoxy]prop-1-en-1-yl)phenyl)isoxazole-3-carboxylic acid
-
5-([(E)-[2-(4-chlorophenyl)-5-oxo-1,3-oxazol-4(5H)-ylidene]methyl]amino)-2-hydroxybenzoic acid
-
-
5-([1-[(2-chloro-1,3-thiazol-5-yl)methyl]-1H-indol-3-yl]methylidene)-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-acetylamino-2-(2,5-dimethyl-1H-pyrrol-1-yl) benzoic acid
-
45% residual activity at 0.1 mM; 46% residual activity at 0.1 mM; 82% residual activity at 0.1 mM; 94% residual activity at 0.1 mM
5-chloro-2-[methyl(methylidene)-lambda4-sulfanyl]-6-[(naphthalen-2-yl)oxy]-1H-benzimidazole
65% inhibition at 0.2 mM
5-chloro-N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-1-methyl-2-(methylthio)-1H-benz-imidazole-6-carboxamide
mixed-type inhibition, complete inhibition at 0.2 mM
5-methoxy-4-[(1E)-3-(4-methoxyphenyl)-3-oxoprop-1-en-1-yl]-2-(2-methylbut-3-en-2-yl)phenyl acetate
-
a semisynthetic licochalcone A derivative
5-[3-bromo-4-[(4-nitrobenzyl)oxy]benzylidene]pyrimidine-2,4,6(1H,3H,5H)-trione
-
-
5-[4-(3,4-dihydroisoquinolin-2(1H)-yl)-3-nitrobenzylidene]-2-thioxodihydropyrimidine-4,6(1H,5H)-dione
-
-
5-[4-[(2-chloro-6-fluorobenzyl)oxy]benzylidene]-1,3-dimethylpyrimidine-2,4,6(1H,3H,5H)-trione
-
-
6,7-dihydroxy-2-(4-hydroxyphenyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
6,8-dibenzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.013 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-((1-(benzylsulfonyl)piperidin-4-yl)amino)-3-(carboxymethoxy)thieno(3,2-b)(1)benzothiophene-2-carboxylic acid
-
-
6-((2-benzyl-1-benzothien-3-yl)methyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0032 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-((E)-1,2-diphenylvinyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0097 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-2-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.006 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0077 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(1-benzothien-3-ylmethyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.06 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0025 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.57 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-(4-((2-benzyl-1-benzothiophen-3-yl)methyl)phenyl)-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.001 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR at 0.52 mM
6-(4-(3-(3-(benzyloxy)-2-(methoxycarbonyl)phenoxy)propyl)piperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of 45.2 mg/ml
6-(4-benzylpiperazin-1-yl)-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
62.3% inhibition at 0.02 mg/ml
6-(9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0071 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-amino-1-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
12.4% inhibition at 0.02 mg/ml
6-benzyl-1-cyclopropyl-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
87.5% inhibition at 0.02 mg/ml
6-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.036 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0043 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-biphenyl-4-yl-4-oxo-8-phenyl-4H-chromene-3-carbaldehyde
50% inhibition at 0.002 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases, 50% inhibition of isoform LAR above 1 mM
6-bromo-3-carboxymethoxy-benzo(b)-thiophene-2-carboxylic acid
-
-
6-bromo-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.020 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-chloro-7-(2,3-dihydro-1H-inden-1-ylamino)quinoline-5,8-dione
-
6-chloro-7-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
-
6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0076 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
6-fluoro-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
35% residual activity at 0.1 mM; 63% residual activity at 0.1 mM; 72% residual activity at 0.1 mM; 75% residual activity at 0.1 mM
6-hydroxy-2-(4-hydroxybenzyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
20% inhibition of PTP-B1 at 0.015 mM
6-hydroxy-2-phenyl-3-((3-trifluoromethyl)phenyl)benzofuran-5-carboxylic acid
-
most potent, reversible and noncompetitive inhibitor, highly selective towards isoform PTPB
6-hydroxy-3-[1-[4-(naphthalen-1-ylamino)-4-oxobutyl]-1H-1,2,3-triazol-4-yl]-2-phenyl-1-benzofuran-5-carboxylic acid
-
-
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylate
-
80% residual activity at 0.1 mM
6-hydroxy-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
38% residual activity at 0.1 mM; 50% residual activity at 0.1 mM; 73% residual activity at 0.1 mM
6-iodo-1-(4-methoxy-3-(methoxycarbonyl)benzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
IC50 of more than 20 mg/ml
6-oxo-6H-cyclohepta[b]furan-5,7-dicarboxylic acid
-
7-(2-((1H-imidazol-2-yl)thio)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
the inhibitor is significantly selective for enzyme protein tyrosine phosphatase 1B (PTP1B) versus other phosphatases, i.e. T-cell protein tyrosine phosphatase (TCPTP), megakaryocyte protein tyrosine phosphatase (PTP-MEG2), and src homology phosphatase 2
7-(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(4-nitro-1H-imidazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-(5-methyl-1H-tetrazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one
-
7-(2-bromoethoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-(3-(4-nitro-1H-imidazol-1-yl)propoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-((1H-imidazol-2-yl)thio)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(1H-1,2,4-triazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(2-methyl-5-nitro-1H-imidazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-(5-methyl-1H-tetrazol-1-yl)butoxy)-2-phenyl-4H-chromen-4-one
-
7-(4-bromobutoxy)-2-phenyl-4H-1-benzopyran-4-one
-
7-bromo-6-difluoromethylphosphonate 3-naphthalenenitrile
50% inhibition at 230 nM for wild-type, at 886 nM for mutant S295F
7-chloro-6-[(2-morpholin-4-ylethyl)amino]quinoline-5,8-dione
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3'',4''-dihydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(3''-carboxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-carboxy-3''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4'-hydroxyphenyl)-3-[(4''-hydroxy-1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
-
7-hydroxy-2-(4-hydroxybenzyl)-4H-chromen-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
7-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-4H-chromen-4-one
-
isolated from the CH2Cl2 extract of Glycyrrhiza inflata
7-hydroxy-2-(4-hydroxyphenyl)-3-[(3',4'-dihydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one
60% inhibition of LMW-PTP isozyme 2, 25% inhibition of LMW-PTP 1, and 50% inhibition of PTP-B1, at 0.02 mM
7-hydroxy-2-(4-hydroxyphenyl)-3-[(4'-carboxy-3'-hydroxy-1,1-biphenyl-3-yl)methyl]-4H-1-benzopyran-4-one
5% inhibition of LMW-PTP isozyme 2, 10% inhibition of LMW-PTP 1, and 59% inhibition of PTP-B1, at 0.02 mM
7-hydroxy-2-(4-hydroxyphenylethyl)-3-[(1,1-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
20% inhibition of PTP-B1 at 0.015 mM
7-hydroxy-2-(4-hydroxyphenylmethyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
10% inhibition of PTP-B1 at 0.015 mM
7-hydroxy-2-(4-hydroxyphenylpropyl)-3-[(1,1'-biphenyl-4-yl)methyl]-4H-1-benzopyran-4-one
10% inhibition of LMW-PTP isozymes 1 and 2,no inhibition of PTP-B1, at 0.015 mM
8-acetyl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
48% residual activity at 0.1 mM; 66% residual activity at 0.1 mM; 81% residual activity at 0.1 mM; 83% residual activity at 0.1 mM
8-benzyl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.018 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-4-carboxylic acid
-
33% residual activity at 0.1 mM; 41% residual activity at 0.1 mM; 8% residual activity at 0.1 mM; 90% residual activity at 0.1 mM
8-bromo-4-oxo-6-(2-phenyl-1-benzothien-3-yl)-4H-chromene-3-carbaldehyde
50% inhibition at 0.0078 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(10-bromo-9-anthryl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.011 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-(2-bromo-1-benzothien-3-yl)-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.0082 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-1-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.010 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-bromo-6-dibenzo(b,d)thien-4-yl-4-oxo-4H-chromene-3-carbaldehyde
50% inhibition at 0.016 mM, irreversible, selective for isoform PTP1B over other human protein tyrosine phosphatases
8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylic acid
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
abietic acid
a nonpolar inhibitor and weak mixed-type inhibitor of PTP1B, inhibits the enzyme by binding to its active site in a nonsubstrate-like manner that stabilizes the catalytically essential WPD loop in an inactive conformation, modelling of enzyme binding. Upon binding to the active site, abietic acid forms a hydrogen bond with R221 that weakens a bond between R221 and E115 and prevents the formation of a hydrogen bond between W179 and R221 that forms when the WPD loop closes
acanthoic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.024 mM
acetaldehyde
-
more than 95% remaining activity at 0.5 mM
Acetylsalicylic acid
-
80% inhibition at 0.2 mM
acrolein
-
4% remaining activity at 0.5 mM, potent irreversible time-dependent inhibitor, addition of 1 mM vanadate slows inactivation of PTP1B by 0.5 mM acrolein
antimonate
-
inhibition of protein tyrosine phosphatase activity
aquastatin A
-
derived from marine fungus Cosmospora sp. SF-5060, competitive inhibition
arsenate
-
inhibition of protein tyrosine phosphatase activity
benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate
-
-
benzyl 1,6-dibenzyl-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
0.1% inhibition at 0.02 mg/ml
benzyl 1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxylate
-
80.5% inhibition at 0.02 mg/ml
benzyl oleanolic acid amide
-
benzyl oleanolic acid ester
-
Berberine
binding structure, molecular modeling, overview
betulinic acid
-
95.1% PTP1B inhibitory activity with 0.0007 mg/ml
betulinic acid methyl ester
-
89.4% PTP1B inhibitory activity with 0.00093 mg/ml
biphenyl-3,4-diol
25% inhibition of LMW-PTP isozyme 2, and 10% inhibition of LMW-PTP 1 and PTP-B1 at 0.02 mM
bis(2-ethyl-maltolato)oxidovanadium(IV)
noncompetitive inhibition of hydrolysis of 4-nitrophenyl phosphate and of phosphorylated undecapeptide substrate EGFR988-998 in the presence of bis(2-ethyl-maltolato)oxidovanadium(IV)
bis(2-methyl-maltolato)oxidovanadium(IV)
-
bis(3-hydroxy-2-methyl-4(1H)pyridinonato)oxidovanadium(IV)
-
bis(acetylacetonato)oxidovanadium(IV)
acts as an uncompetitive inhibitor of PTP1B with DADEpYLIPQQG as the substrate, but this VO2+-chelate exhibits only apparent competitive inhibition of 4-nitrophenyl phosphate hydrolysis when catalyzed by PTP1B, differing from that observed in the hydrolysis of the phosphotyrosine-containing undecapeptide DADEpYLIPQQG mimicking residues 988-998 of the epidermal growth factor receptor (EGFR). Addition of 4-nitrophenyl phosphate after addition of saturating amounts of bis(acetylacetonato)oxidovanadium(IV) to PTP1B causes complete loss of catalytic activity
cantharidin
-
17% inhibition at 1 mM
chloro(1,3-dimethyl-1,3-dihydro-2H-imidazol-2-ylidene)gold
-
i.e. [(p-MeMeIm)AuICl]
chloro(1-methyl-1,3-dihydro-2H-imidazol-2-ylidene)gold
-
i.e. [(MeIm)AuICl]
chloro[1-methyl-3-(4-methylbenzyl)-2,3-dihydro-1H-imidazol-2-yl]gold
-
i.e. [(p-MeBzMeIm)AuICl]
continentalic acid
modelling of enzyme binding
corosolic acid
-
50% inhibition at 0.0072mM, mixed-type inhibition
Cr(VI)
-
as Na2CrO4, induces clonogenic lethality
crotonaldehyde
-
85% remaining activity at 0.5 mM
cyclopropyl-6-(4-fluorobenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
-
71.1% inhibition at 0.02 mg/ml
dehydroabietic acid
modelling of enzyme binding
dehydrocostuslactone
-
86.2% PTP1B inhibitory activity with 0.00651 mg/ml
diethylcarbamazine
-
12% inhibition at 0.2 mM
diethyldicarbonate
-
7% inhibition at 1 mM
Differentiation inducing factor 1
-
DIF-1, inhibits PTP3 by induction of serine-threonine phosphorylation of PTP3
-
dihydroabietic acid
modelling of enzyme binding
disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition at 0.030 mM, reversible and competitive
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
DTT
-
inhibition of cytosolic enzyme form
dysidiolide
inhibits Cdc25A
EDTA
-
51% inhibition at 5 mM
ent-17-hydroxykaur-15-en-19-oic acid
40% inhibition at 0.033 mM
ent-3beta-angeloyloxykaur-16-en-19-oic acid
-
ent-3beta-tigloyloxykaur-16-en-19-oic acid
-
ent-kaur-16-en-19-oic acid
-
diterpenoid isolated from Acanthopanax koreanum, 50% inhibition at 0.020 mM
ent-kaur-9(11),16-dien-19-oic acid
29% inhibition at 0.033 mM
erylysins A
-
i.e. 3''-hydroxy-2',2'-dimethylpyrano[6',5':3,4]-2'',2''-dimethyldihydropyrano[6'',5'':9,10]pterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1
erylysins B
-
i.e. furano[5',4':3,4]-9-hydroxy-10-prenylpterocarpan, a pterocarpan isolated from stem bark of Erythrina lysistemon, inhibits PTPB1
ethyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-6,6,10a,12a-tetramethyl-1,2,3,3a,3b,4,6,6a,7,9a,10,10a,10b,11,12,12a-hexadecahydrocyclopenta[5,6]naphtho[1,2-f]indazol-1-yl]pentanoate
-
-
ethyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-8-amino-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinazolin-1-yl]pentanoate
-
-
ethyl 4-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]butanoate
-
-
ethyl [4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetate
-
-
FlAsH
the small molecule biarsenical fluorescein derivative, FlAsH, is no inhibitor of the wild-type enzyme but of the engineered WPD insertion mutant enzyme that displays FlAsH-binding cysteine residues. Inhibition of the FlAsH-sensitized TCPTP mutants is rapid and specific, and strong FlAsH sensitivity is observed in mutants that contain as few as two cysteine point mutations in their engineered WPD loops, minimization of FlAsH-binding determinants, overview
fluorescein arsenical hairpin binder
fluorescein arsenical hairpin binder does not inhibit any wild type PTP, but insertion of a fluorescein arsenical hairpin binder-binding peptide (CCPGCC) at a conserved position in the PTP catalytic-domain's WPD loop confers fluorescein arsenical hairpin binder sensitivity upon divergent PTPs
-
Glyoxal
-
93% remaining activity at 0.5 mM
glyoxalbis(N(4)-methylthiosemicarbazonato)Cu(II)
-
inhibition of protein tyrosine phosphatase activity is the prerequisite for activation of epidermal growth factor receptor by the compound, overview
hexadecanoyl-5-hydroxymethyl tetronic acid
potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR; potent irreversible inhibitor of VHR
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
isopimaric acid
modelling of enzyme binding
L-(+)-Tartrate
-
6.5% inhibition at 5 mM
lithocholic acid
-
natural inhibitor against PTP1B
lobaric acid
-
a depsidone-type compound, isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
lupenone
-
isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner
lupeol
-
isolated from Sorbus commixta stem bark, inhibits PTP1B in a selective and noncompetitive manner
menadione
inhibits Cdc25B irreversibly
methyl (4R)-4-[(1R,3aS,3bS,10aR,10bS,12aR)-8-amino-6,6,10a,12a-tetramethyl-2,3,3a,3b,4,6,10,10a,10b,11,12,12a-dodecahydro-1H-cyclopenta[7,8]phenanthro[2,3-d][1,3]thiazol-1-yl]pentanoate
-
-
methyl (4R)-4-[(1R,3aS,3bS,11aR,11bS,13aR)-6,6,11a,13a-tetramethyl-2,3,3a,3b,4,6,11,11a,11b,12,13,13a-dodecahydro-1H-cyclopenta[5,6]naphtho[1,2-g]quinoxalin-1-yl]pentanoate
-
-
methyl (6S,10S)-12-(2-chloro-3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-(2-fluoro-5-iodobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-(2-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-(3,4-dichlorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-(3,4-difluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-(3-bromo-4-fluorobenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-(3-hydroxybenzyl)-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-benzyl-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-12-[(4,6-dichloro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-[(4-chloro-6-fluoro-2H-chromen-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA, inhibition kinetics, overview
methyl (6S,10S)-12-[(5-chloro-1H-indol-3-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-12-[(5-methylfuran-2-yl)methyl]-9-oxo-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
absolutely specific for MptpB, no inhibition of MptpA
methyl (6S,10S)-9-hydroxy-12-(3-hydroxybenzyl)-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl (6S,10S)-9-oxo-12-(pyridin-3-ylmethyl)-6,7,8,9,10,11-hexahydro-5H-6,10-epiminocycloocta[b]indole-8-carboxylate
-
-
methyl 2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 2-(3-(1-(4-fluorobenzyl)-6-nitro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate
-
IC50 of 6.5 mg/ml
methyl 2-(3-(1-benzyl-7-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamido)propoxy)-6-hydroxybenzoate
-
IC50 of 9.4 mg/ml
methyl 2-[4-[(4-[[ethoxy(oxo)acetyl][2-(methoxycarbonyl)phenyl]amino]-3-ethylphenylalanyl)amino]butoxy]-6-hydroxybenzoate
-
methyl 3,8-dimethoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 3-formyl-2,4-dihydroxy-6-methylbenzoate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl 4,4-dimethyl-3-oxochol-5-en-24-oate
-
-
methyl 4-[(benzylseleninyl)methyl]-N-(tert-butoxycarbonyl)-L-phenylalaninate
-
-
methyl 5-amino-6-(7-amino-6-methoxy-5,8-dioxo-5,8-dihydroquinolin-2-yl)-4-(2-hydroxy-3,4-dimethoxyphenyl)-3-methylpyridine-2-carboxylate
-
methyl 8-hydroxy-3-methoxy-11-oxo-1-pentanoyl-6-pentyl-11H-dibenzo[b,e][1,4]dioxepine-7-carboxylate
-
isolated from a methanol extract of the Antarctic lichen Stereocaulon alpinum
methyl N-(tert-butoxycarbonyl)-4-(hydroxymethyl)-L-phenylalaninate
-
-
methyl N-(tert-butoxycarbonyl)-4-[(5R)-5-(methoxycarbonyl)-9,9-dimethyl-7-oxo-8-oxa-3-thia-2-selena-6-azadec-1-yl]-L-phenylalaninate
-
-
methyl oleanolic acid amide
-
methyl oleanolic acid ester
-
methyl-5-((3-(benzylcarbamoyl)-6-iodo-4-oxoquinolin-1(4H)-yl)methyl)-2-methoxybenzoate
-
IC50 of more than 20 mg/ml
mokko lactone
-
93.1% PTP1B inhibitory activity with 0.00141 mg/ml
mpV(pic)
-
potent and selective PTP inhibitor, inhibits SPH-1 in a dose-dependent manner
MSI-1436
small molecule inhibitor MSI-1436 binds to the disordered C-terminal domain of PTP1B, C-terminal to the catalytic domain, MSI-1436 functions using an allosteric mechanism to direct the enzymatic activity of PTP1B
N,1-dibenzyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
41.4% inhibition at 0.02 mg/ml
N,1-dibenzyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
61.8% inhibition at 0.02 mg/ml
N,N'-[benzene-1,4-diylbis(propane-2,2-diylbenzene-4,1-diyl)]bis(1,1,1-trifluoromethanesulfonamide)
-
-
N-((4-((E)-2-nitroethenyl)phenyl)carbonyl)glycyl-L-alpha-glutamyl-L-glutamic acid
-
50% inhibition at 0.0014 mM in absence of 2-mercaptoethanol, at 0.275 mM in presence of 1 mM 2-mercaptoethanol
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-a-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
inhibition of enzyme increases caveolin-1 phosphorylation
N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalaninamide
-
-
N-(1,4-dioxo-1,4-dihydronaphthalen-2-yl)-N-(4-methylphenyl)acetamide
-
N-(3-chloro-4-fluorophenyl)-2-[(6,7-dimethoxy-4-oxo-3-phenyl-3,4-dihydro-2-quinazolinyl)sulfanyl]acetamide
80% inhibition at 0.2 mM
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
N-(3-[(3,5-difluorobenzyl)oxy]pyridin-2-yl)-4-pentylbenzenesulfonamide
74% inhibition at 0.2 mM
N-(3-[(4-chlorophenyl)sulfanyl]-1,4-dioxo-1,4-dihydronaphthalen-2-yl)acetamide
-
N-(4-([(6-ethoxy-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide
-
-
N-(4-([(6-methoxy-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide
-
-
N-(4-([(6-methyl-1,3-benzothiazol-2-yl)amino]sulfonyl)phenyl)acetamide
-
-
N-(4-[[(6-nitro-1,3-benzothiazol-2-yl)amino]sulfonyl]-phenyl)acetamide
-
-
N-(6-chloro-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-methoxybenzenesulfonamide
-
-
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-methylbenzenesulfonamide
-
-
N-(6-ethoxy-1,3-benzothiazol-2-yl)-4-nitrobenzene sulfonamide
-
linear mixed-type inhibition, shows in vivo antihyperglycemic activity
N-(6-ethoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
N-(6-fluoro-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
N-(6-methoxy-1,3-benzothiazol-2-yl)-4-methylbenzenesulfonamide
-
-
N-(6-methoxy-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
-
N-(6-methoxy-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
N-(6-methyl-1,3-benzothiazol-2-yl)-4-nitrobenzenesulfonamide
-
linear mixed-type inhibition, shows in vivo antihyperglycemic activity
N-(6-methyl-1,3-benzothiazol-2-yl)benzenesulfonamide
-
-
N-([4-[difluoro(phosphono)methyl]phenyl]acetyl)-a-aspartyl-4-[difluoro(phosphono)methyl]phenylalaninamide
-
-
N-1-(2-[(2-oxo-4-propyl-2H-chromen-7-yl)oxy]propanoyl)-3-(trifluoromethyl)benzene-1-sulfonohydrazide
84% inhibition at 0.2 mM
N-benzoyl-L-glutamyl-[4-phosphono(difluoromethyl)]-L-phenylalanineamide
-
i.e. BzN-EJJ-amide, 50% inhibition at 4 nM
N-benzyl-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
0.2% inhibition at 0.02 mg/ml; 7.4% inhibition at 0.02 mg/ml
N-benzyl-1-cyclopropyl-6-iodo-4-oxo-1,4-dihydroquinoline-3-carboxamide
-
6.1% inhibition at 0.02 mg/ml
n-dodecyl trimethylammonium bromide
-
pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration
n-hexadecyl trimethylammonium bromide
-
pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration
N-Methylmaleimide
-
76.3% inhibition at 0.5 mM
n-tetradecyl trimethylammonium bromide
-
pH 7.0, inactivation at concentration 10fold higher than critical micellar concentration
N-[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenyl]-4-tert-butylbenzamide
-
-
N-[5-(dimethylamino)-2-hydroxy-3-methoxybenzyl]-N-methyl-2-(4-nitrophenyl)ethanaminium
-
N-[6-chloro-5-(2,3-dichlorophenoxy)-1-methyl-1H-benzimidazol-2-yl]acetamide
70% inhibition at 0.2 mM
N-[6-chloro-5-(2,3-dichlorophenoxy)-1H-benzimidazol-2-yl]-2,2,2-trifluoroacetamide
mixed-type inhibition, 92% inhibition at 0.2 mM
N2-(2-((2-((N-((4-(difluoro(phosphono)methyl)phenyl)acetyl)-L-alpha-aspartyl-4-(difluoro(phosphono)methyl)-L-phenylalanyl)amino)ethyl)disulfanyl)ethyl)-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-arginyl-D-argininamide
-
in presence of 5-50 nM, 11-35% decrease in cell spreading, 24% decrease in number of migratory cells, dose-dependent increase in Y527 phosphorylation of Src
Na+/K+ tartrate
-
20% residual activity in ovary and 2% residual activity in haemolymph at 10 mM
NO
-
inactivation, phosphate protects
nocardione A
inhibits Cdc25B
nocardione B
inhibits Cdc25B
NSC-87877
-
potent Shp2 and Shp1 inhibitor
p-chloromercuribenzoate
-
lung enzyme
p-hydroxymercuribenzoate
-
p-nitrocatechol sulfate
-
competitive inhibitor
PAO
complete inhibition at 0.0.5 mM
papaverine
binding structure, molecular modeling, overview
peracetic acid
-
a potent, time-dependent inactivator of the catalytic subunit of PTP1B, treatment of the enzyme with 0.015 mM for 15 sec inactivates 88% of the enzyme, inactivation of PTP1B by peracetic acid can be reversed by treatment of the enzyme with thiols
phenyl vinyl sulfonate
-
phenyl vinyl sulfonate-mediated PTP inactivation is active site-directed and irreversible
phenyl vinyl sulfone
-
phenyl vinyl sulfone-mediated PTP inactivation is active site-directed and irreversible
phenylhydrazonopyrazolone sulfonate 1
-
potent, active site-directed small molecule inhibitor which is specific for Shp2 over the closely related tyrosine phosphatases Shp1 and PTP1B
phenylhydrazonopyrazolone sulfonate 4
-
the most potent inhibitor of Shp2 which shows a specificity profile similar to phenylhydrazonopyrazolone sulfonate 1
potassium bisperoxo(1,10-phenanthroline)oxovanadate
potassium bisperoxo(1,10-phenanthroline)oxovanadate(V)
-
i.e. [bpV(phen)], the peroxovanadium compound is a stable, potent and selective protein tyrosine phosphatase inhibitor. It protects dorsal column sensory axons and white matter and rescues sensory-evoked potentials in vivo after treatement with PTP or spinal cord injury, overview
propanal
-
93% remaining activity at 0.5 mM
pterokaurene L3
no inhibition at 0.031 mM
regucalcin
-
regulatory protein in intracellular signaling
-
rilobolide-6-O-methacrylate
no inhibition at 0.026 mM
S-nitrosoglutathione
-
S-nitrosoglutathione treatment decreases the catalytic activity parameters of PtpA by half
SK7
-
a metal chalcone, complete inhibition at 0.02 mM
small t antigen
-
small t antigen of DNA tumor virus SV40 inhibits the phosphatase activity of the PP2A core enzyme
-
sodium decylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
Sodium diphosphate
-
both isoforms, inhibition by millimolar concentrations
sodium dodecylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
sodium octylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
sodium pervanadate
-
broad-acting tyrosine phosphatase inhibitor
Sodium tetradecylsulfate
-
at concentration 10fold lower than critical micellar concentration, complete inactivation. Inactivation is independent of pH-value, irreversible and not affected by NaCl. Presence of phosphate protects
sodium tungstate
-
complete inhibition of enzyme isolated from metacyclic stage, 50% inhibition of enzyme from procyclic stage
stevastelin
inhibits VHR; inhibits VHR; inhibits VHR
sulfircin
inhibits Cdc25A
Tartrate
-
both SynPPP1 and SYnPPM3
tetramisole
-
both SynPPP1 and SYnPPM3
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
Trifluoperazine
-
complete inhibition of enzyme isolated from metacyclic stage, 18% inhibition of enzyme from procyclic stage
trilobolide-6-O-isobutyrate
no inhibition at 0.026 mM
VO3N3
-
oxovanadium(IV) is coordinated with one nitrogen and two oxygen atoms from the Schiff base and two nitrogen atoms from the bidentate planar ligands, in a distorted octahedral geometry, VO3N3
wedelolide D
32% inhibition at 0.020 mM
wedelolide H
no inhibition at 0.023 mM
wedelolide I
no inhibition at 0.021 mM
wedelolide J
no inhibition at 0.021 mM
[(1-benzyl-1H-indazol-5-yl)(difluoro)methyl]phosphonic acid
-
[(2-benzyl-2H-indazol-5-yl)(difluoro)methyl]phosphonic acid
-
[(4-bromophenyl)(difluoro)methyl]phosphonic acid
-
[(4-[(4E)-2-(1H-benzotriazol-1-yl)-2-[4-(methoxycarbonyl)phenyl]-5-phenylpent-4-en-1-yl]phenyl)(difluoro)methyl]phosphonic acid
-
[(4-[[3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
-
[(4-[[4-bromo-3,5-bis(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
selectivity with different PTPs, overview
[(4-[[4-bromo-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
-
[(4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)(difluoro)methyl]phosphonic acid
-
[(BzMeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[(MeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[(MeMeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[(p-MeBzMeIm)Au(I)Cl]
Yersinia enterolytica
-
-
[2-bromo-4-[(E)-(7,8-dimethyl-3-oxo[1,3]thiazolo[3,2-a]benzimidazol-2(3H)-ylidene)methyl]-6-ethoxyphenoxy]acetic acid
irreversible inhibition
[4-[(2E)-3-(5-bromo-4-hydroxy-2-methoxyphenyl)prop-2-enoyl]phenoxy]acetic acid
-
-
[biphenyl-4-yl(difluoro)methyl]phosphonic acid
-
[difluoro(4-nitrophenyl)methyl]phosphonic acid
-
[difluoro(4-[[2-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro(4-[[3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro(4-[[4-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro(4-[[4-fluoro-3-(trifluoromethyl)phenyl]carbamoyl]phenyl)methyl]phosphonic acid
-
[difluoro[3-(phenylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(1,3-thiazol-2-ylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(1-methyl-1H-pyrazol-4-yl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(methylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(phenoxymethyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(phenylcarbamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(phenylsulfamoyl)phenyl]methyl]phosphonic acid
-
[difluoro[4-(propan-2-ylcarbamoyl)phenyl]methyl]phosphonic acid
-
[RuIII(EDTA)(OH2/OH)]1-/2-
-
RuIII-EDTA inhibits PTP, like vanadate, through an oxidant-independent pathway. It inhibits PTP at physiological pH values by a mechanism that involves binding of the Cys residue of the catalytic domain of the enzyme, overview. At pH 7.4, the Ru-EDTA complex exists as a mixture of aqua and hydroxo-species. The inhibition is reversible or inhibited by glutathione
-
[[1-(4-chlorophenyl)-2-methyl-1H-indol-5-yl]oxy]acetic acid
-
[[4'-(2-butyl-1-benzofuran-3-yl)biphenyl-4-yl]oxy]acetic acid
-
[[4-(1H-benzimidazol-2-ylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid
-
[[4-(benzoylamino)phenyl](difluoro)methyl]phosphonic acid
-
[[4-(benzylcarbamoyl)phenyl](difluoro)methyl]phosphonic acid
-
[[4-([[3,5-bis(trifluoromethyl)phenyl]carbamoyl]amino)phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(1-ethylpiperidin-4-yl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(2-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(2-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(3-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(3-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(4-bromophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
[[4-[(4-chlorophenyl)carbamoyl]phenyl](difluoro)methyl]phosphonic acid
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
-
-
(4aS,6aS,6bR,14aR)-2,2,6a,6b,9,9,14a-heptamethyl-1,3,4,5,6,6a,6b,7,8,8a,9,14,14a,14b,15,16b-hexadecahydrochryseno[1,2-g]quinazoline-4a(2H)-carboxylic acid
no inhibition of LMW-PTP isozymes, but 20% inhibition of PTP-B1 at 0.02 mM
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
-
covalent mode of action
1-ethyl-6-methyl-3-phenyl-1H-pyrimido(5,4-e)(1,2,4)triazine-5,7-dione
-
covalent mode of action
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
-
competitive, noncovalent mode of action
2,2-dioxo-2,3-dihydro-2-OMEGA-16-benzo (1,2,3)oxathiazole-6-carboxylic acid (5-phenylsulfanyl-1H-benzoimidazol-2-ylmethyl)-amide
-
competitive, noncovalent mode of action
Ag+
-
16.6% inhibition at 2 mM
Ag+
-
62% inhibition at 2.5 mM
Ammonium molybdate
-
complete inhibition of enzyme isolated from metacyclic stage, 75% inhibition of enzyme from procyclic stage
Ammonium molybdate
-
4% residual activity in ovary and no activity in haemolymph at 1 mM
Ammonium molybdate
-
98% inhibition at 2 mM
Ammonium molybdate
-
strong inhibition
auranofin
-
inhibition of cysteine-dependent protein tyrosine phosphatases
auranofin
Yersinia enterolytica
-
inhibition of cysteine-dependent protein tyrosine phosphatases
BzN-EJJ-amide
50% inhibition at 3.7 nM for wild-type, at 18 nM for mutant S295F
BzN-EJJ-amide
-
50% inhibition at 8nM for wild-type PTP-1B, at 14 nM for PTP-1B mutant V113I, at 7 nM for mutant M114V, at 7 nM for mutant V113I/M114V, at 11 nM for mutant G117E, at 12 nM for mutant L119V
Ca2+
-
-
CinnGel 2ME
-
30.2% inhibition at 0.02 mM
CinnGel 2ME
-
the free cinnamic acid component of CinnGEL 2Me inhibits PTP1B
Cu2+
-
lung enzyme
Cu2+
Bracoviriform demolitoris
-
-
Cu2+
-
32.2% inhibition at 2 mM
dephostatin
-
complete inhibition of enzyme isolated from metacyclic stage, 28% inhibition of enzyme from procyclic stage
diphosphate
-
1 mM, 31% residual activity
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.010 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
disodium 4-(((4-methyl-3-(((3-(((3-((2-methyl-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition at 0.012mM, reversible and competitive
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0096 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
disodium hydrogen (3-(((4-(((4-((3-(hydroxyphosphinato)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)phosphonate
-
suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive
dithiothreitol
-
dithiothreitol
complete inhibition at 1.8 mM
Fe2+
-
lung enzyme
Fe2+
-
34.5% inhibition at 2 mM
H2O2
-
inactivation, phosphate protects, mechanism, overview
H2O2
-
the enzyme can be more rapidly inactivated by H2O2 in the absence of EDTA
H3VO4
-
-
H3VO4
-
no effect on PTP-I but PTP-III inhibited
heparin
Bracoviriform demolitoris
-
-
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.005 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8,8'-(((2E)-1,4-dioxobut-2-ene-1,4-diyl)bis(iminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.008mM, reversible and competitive
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0023 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8,8'-(benzene-1,3-diylbis(carbonyliminobenzene-3,1-diylcarbonylimino(4-methylbenzene-3,1-diyl)carbonylimino))dinaphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.0015M, reversible and competitive
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((2'-(((3'-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)biphenyl-2-yl)carbamoyl)amino)biphenyl-4-yl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.020 mM, reversible and competitive
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0037 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((3-methyl-4-(((3-(((3-((2-methyl-4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.007 mM, reversible and competitive
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0021 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((3-methyl-4-(((4-(((4-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.0028mM, reversible and competitive
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0016 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-(((3-(((3-((4-((4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.002mM, reversible and competitive
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-(1-methylethyl)-3-(((3-(((3-((2-(1-methylethyl)-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.013M, reversible and competitive
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.009 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-ethyl-3-(((3-(((3-((2-ethyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.011M, reversible and competitive
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.007 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-(((4-tert-butyl-3-(((3-(((3-((2-tert-butyl-5-((4,5,8-trisulfonatonaphthalen-1-yl)carbamoyl)phenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)phenyl)carbonyl)amino)naphthalene-1,4,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.013M, reversible and competitive
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.00049 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
hexasodium 8-([[2-(3-[[(3-[5-[(4,6,8-trisulfonatonaphthalen-1-yl)carbamoyl]-1H-benzimidazol-2-yl]phenyl)carbamoyl]amino]phenyl)-1H-benzimidazol-5-yl]carbonyl]amino)naphthalene-1,3,5-trisulfonate
-
suramin-derivative, 50% inhibition at 0.00009M, reversible and competitive
iodoacetic acid
-
-
iodoacetic acid
-
complete inhibition at 1.0 mM
ISIS 113715
-
PTP-1B antisense oligonucleotide ISIS 113715 dose-dependently inhibits PTP-1B mRNA and protein expression, although ISIS 113715 reduces PTP-1B protein levels by greater than 90%, no effects are observed on protein levels of TC-PTPase
-
ISIS 113715
-
PTP-1B antisense oligonucleotide ISIS 113715 administration reduces PTP-1B mRNA expression in both liver and adipose tissue by 40-50% but does not affect muscle PTP-1B expression
-
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl)([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview. The inhibitor shows a hypoglycaemic effect in ob/ob mice, overview
JTT-551
-
i.e. monosodium (([5-(1,1-dimethylethyl)thiazol-2-yl]methyl) ([(4-(4-[4-(1-propylbutyl)phenoxy]methyl)phenyl)thiazol-2-yl]methyl)amino)acetate, a specific protein tyrosine phosphatase 1B inhibitor in vitro and in vivo, mixed-type inhibition mode versus PTPB1, overview. The inhibitor shows a hypoglycaemic effect in rat L6 cells, overview
L-Tartrate
-
no inhibition of lung enzyme
L-Tartrate
-
no inhibition of platelet enzyme
maslinic acid
-
poor inhibition by the isomers 3-epi-maslinic acid and augustic acid
Mg2+
-
-
Mn2+
-
-
Mn2+
-
no inhibition of platelet enzyme
molybdate
-
-
molybdate
competitive inhibition
molybdate
-
92.2% inhibition at 5 mM
molybdate
-
no effect on PTP-I, PTP-III inhibited
molybdate
-
competitive inhibition
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
-
suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR
N-(3-formylphenyl)-3-(((3-((3-formylphenyl)carbamoyl)phenyl)carbamoyl)amino)benzamide
-
suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive
N-ethylmaleimide
-
-
N-ethylmaleimide
-
both isozymes, 50% inhibition at 7 mM
Na3VO4
-
-
NaCl
-
increase in Km-value with increase of ionic strength, 10-fold increase of Km-value from 0 to 200 mM NaCl
NaCl
-
inhibits activity with 4-nitrophenyl phosphate
NaCl
inhibits the catalytic domain by 60% at 2 M
NaF
-
1 mM, 85% residual activity
NaF
-
no inhibition of lung enzyme
NaF
-
no inhibition of platelet enzyme
NaF
-
16% residual activity in ovary and no activity in haemolymph at 10 mM
NaF
-
moderate inhibition, both SynPPP1 and SYnPPM3
o-vanadate
Na3VO4, complete inhibition at 0.6 mM
o-vanadate
-
both SynPPP1 and SYnPPM3
okadaic acid
-
complete inhibition of enzyme isolated from metacyclic stage, 35% inhibition of enzyme from procyclic stage
okadaic acid
-
7.5% inhibition at 0.01 mM
okadaic acid
-
both SynPPP1 and SYnPPM3
oleanolic acid
-
orthovanadate
-
-
orthovanadate
competitive inhibitor
orthovanadate
-
inhibition of protein tyrosine phosphatase activity
orthovanadate
-
24.5% inhibition at 5 mM
orthovanadate
Q6JHV2
50% inhibition at 0.075 mM
pervanadate
-
-
pervanadate
-
pervanadate inhibits PTP by irreversibly oxidizing the catalytic cysteine of PTP
Phenylarsine oxide
-
specific inhibitor of protein Tyr phosphatase activity
Phenylarsine oxide
-
55.8% inhibition at 0.01 mM
Phenylarsine oxide
-
a specific PTP inhibitor, 79% inhibition at 1.0 nM
phosphate
-
-
phosphate
inhibits the phosphatase activity, but not the sugar hydrolase activity; inhibits the phosphatase activity, but not the sugar hydrolase activity
phosphate
-
38% residual activity in ovary and 3% residual activity in haemolymph at 10 mM
phosphotyrosine
-
-
PO43-
-
treatment of the enzyme with 0.05 mM PO43- for 15 sec inactivates 49% of the enzyme
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
-
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
complete inhibition at 0.01 mM
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
-
potassium bisperoxo(1,10-phenanthroline)oxovanadate
-
potent PTP inhibitor
RK-682
-
-
RK-682
-
98.5% PTP1B inhibitory activity with 0.0012 mg/ml
Sodium fluoride
NaF, 30% inhibition at 5 mM, no inhibition at 1-3 mM
Sodium fluoride
-
96% inhibition at 2 mM
sodium orthovanadate
-
17.5% inhibition at 1 mM
sodium orthovanadate
-
a broad-range PTP inhibitor, abrogated Cr(VI)-induced clonogenic lethality
sodium orthovanadate
-
complete inhibition of enzyme isolated from metacyclic stage, 30% inhibition of enzyme from procyclic stage
sodium orthovanadate
-
20% residual activity in ovary and 13% residual activity in haemolymph at 0.1 mM
sodium orthovanadate
-
shows dose-dependent inhibition of PRL activity
sodium orthovanadate
-
99.5% inhibition at 0.05 mM
sodium orthovanadate
-
both isozymes, 50% inhibition at 3 mM
sodium orthovanadate
-
strong inhibition
Sodium vanadate
-
1 mM, 60-80% inhibition
Sodium vanadate
a PTP inhibitor targeting the catalytic site pocket. Vanadate is anchored in the active site of Tk-PTP(form II), stabilized by electrostatic interaction with the guanidinium group of Arg109 and by its oxygen atom-mediated hydrogen bonds with the main chain amides of Met94, Gly95, Leu97, Gly98, and Arg99. The Tk-PTP(form II) P-loop is structurally similar to those of catalytically active DUSP proteins
suramin
-
50% inhibition of PTP1B at 0.011 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
suramin
-
50% inhibition at 0.007M, reversible and competitive
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.00025 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 2-(((2-(3-(((3-(5-((2,5-disulfonatophenyl)carbamoyl)-1H-benzimidazol-2-yl)phenyl)carbamoyl)amino)phenyl)-1H-benzimidazol-5-yl)carbonyl)amino)benzene-1,4-disulfonate
-
suramin-derivative, 50% inhibition at 0.0007mM, reversible and competitive
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B above 0.1 mM, reversible and competitive. Not inhibitory to PTPalpha, CD45 or LAR
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition above 0.1 mM, reversible and competitive
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.08 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4,4'-(benzene-1,3-diylbis(carbonyliminobenzene-4,1-diylcarbonylimino))dinaphthalene-2,6-disulfonate
-
suramin-derivative, 50% inhibition at 0.045 mM, reversible and competitive
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition of PTP1B at 0.0045 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4-(((3-(((3,5-bis((4-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)-5-((4-sulfonatophenyl)carbamoyl)phenyl)carbonyl)amino)benzenesulfonate
-
suramin-derivative, 50% inhibition at 0.005mM, reversible and competitive
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
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suramin-derivative, 50% inhibition of PTP1B at 0.070 mM, reversible and competitive. Not inhibitory to PTPalpha or LAR
tetrasodium 4-(((3-(((5-((4,8-disulfonatonaphthalen-1-yl)carbamoyl)-2-methylphenyl)carbamoyl)amino)-4-methylphenyl)carbonyl)amino)naphthalene-1,5-disulfonate
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suramin-derivative, 50% inhibition at 0.0042 mM, reversible and competitive
tungstate
competitive inhibition
tungstate
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16.3% inhibition at 20 mM
tungstate
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competitive inhibition
ursolic acid
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50% inhibition at 0.0038 mM, competitive inhibition
ursolic acid
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99% PTP1B inhibitory activity with 0.0007 mg/ml
vanadate
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competitive, 1 mM, 11% residual activity
vanadate
Bracoviriform demolitoris
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vanadate
the equatorial vanadate oxygen atoms bind to the P-loop and assumes a trigonal bipyramidal geometry in both transition state analogue structures, with very similar apical O-O distances, binding structure, overview
vanadate
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enzyme inhibition by vanadate takes place through an oxidant-independent pathway, the inhibition is reversible with EDTA
Zn2+
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-
Zn2+
low nanomolar Zn2+ concentrations inhibit isoform PTB1Bll
Zn2+
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75.2% inhibition at 5 mM
Zn2+
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65.5% inhibition at 2.5 mM
Zn2+
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Zn2+ inhibits the enzyme irreversibly in a concentration-dependent manner
additional information
Bracoviriform demolitoris
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the enzyme activity is diminished by increasing acetate buffer ionic strength, but PTP-H2 is unaffected by tetramisole and levamisole, as well as by okadaic acid, sodium fluoride and sodium citrate
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additional information
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hyperosmotic stress inhibits PTP3. Overexpression of a dominant inhibitor of PTP3 leads to constitutive tyrosine phosphorylation and ectopic nuclear localisation of STATc
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additional information
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overview on recently developed inhibitors
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additional information
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inhibition data for isoforms CD45, Cdc25A, VHR; not inhibitory to PTP1B, CD45: disodium 3-(((4-methyl-3-(((2-methyl-5-((3-sulfonatophenyl)carbamoyl)phenyl)carbamoyl)amino)phenyl)carbonyl)amino)benzenesulfonate
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additional information
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enzyme is active in unstimulated or thrombin-stimulated platelets. Enzyme is not active in lysate of platelets adherent to fibrinogen
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additional information
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down-regulation of enzyme activity with small molecule inhibitors suppresses cell spreading and migration to fibronectin, increases Y527 phosphorylation in Src, and decreases phosphorylation of focal adhesion kinase, p130 Crk-associated substrate, and extracellular signal-regulated kinase 1/2
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additional information
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the presence of the superoxide- and hydrogen peroxide-destroying enzymes superoxide dismutase and catalase has no effect on the rate of the inactivation reaction
-
additional information
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tert-butyl hydroperoxide cumene hydroperoxide do not inactivate PTP1B, 150 nM H2O2 has no measurable effect on enzyme activity
-
additional information
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3alpha,24,29-trihydroxyolean-12-en-28-oic acid, 3alpha,19alpha-dihydroxyurs-12,20(30)-dien-24,28-dioic acid, and 3alpha,19alpha-dihydroxyurs-12-en-24,28-dioic acid show very weak inhibitory effect towards PTP1B
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additional information
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not inhibited by costunolide, 11beta,13-dihydrocostunolide, reynosin, 1beta-hydroxy arbusculin A, santamarine, alpha-costol, beta-sitosterol, aplotaxene, and alpha-amyrin stearate
-
additional information
no inhibition by EDTA at 1 mM
-
additional information
structure derivatives, derived from papaverine, e.g. Pnu177496, in docking simulations, simulated molecular docking method, overview
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additional information
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structure derivatives, derived from papaverine, e.g. Pnu177496, in docking simulations, simulated molecular docking method, overview
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additional information
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inhibitor synthesis, inhibitor selectivity for PTP1B over TCPTP, overview
-
additional information
structure-based optimization of benzoic acids as inhibitors of PTPB1 and LMW-PTP, molecular docking study using crystal structures of PTPB1, PDB ID 1G7G and 1XBO, as templates, overview
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additional information
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synthesis of series of oxovanadium complexes with mixed ligands, a tridentate ONO-donor Schiff base ligand with salicylidene anthranilic acid, and a bidentate NN ligand, e.g., 2,2'-bipyridine, 1,10-phenanthroline, dipyrido[3,2-d:2',3'-f]quinoxaline, dipyrido[3,2-a:2',3'-c]phenazine, or 7-methyldipyrido[3,2-a:2',3'-c]phenazine, spectroscopical analysis, and crystal structures of complexes bound to PTPB1, molecular modeling, overview
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additional information
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mechanism of substrate selectivity of five bidentate inhibitors, NNY, B07, F6Z, Q1M, and PYN, for PTP1B, compared to SHP-2 and TCPTP, using molecular dynamics simulations and free energy calculations, and crystal structures with PDB IDs 1NNY, 2B07, 2F6Z, 1Q1M, and 1PYN, 1L8k, and 2SHP, overview. Residues Arg24, Arg254, and Gln262 in the second binding site of PTP1B are essential for the high selectivity of inhibitors
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additional information
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inhibitory potency of gold(I) complexes containing N-heterocyclic carbene ligands versus cysteine-dependent protein tyrosine phosphatases, reversible inhibition, overview
-
additional information
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bis(thiosemicarbazonato) metal complexes, e.g. with Cu2+ or Zn2+, inhibit PTP and its dephophorylating and inhibitory activity on the epidermal growth factor receptor, EGFR
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additional information
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the substitution of prenyl groups on pterocarpans might be important for in vitro PTP1B inhibitory activity, and hydroxyl group attached to C-6a or an aldehyde group attached to C-8 may decrease this activity. No inhibition by erylysins C, i.e. 8-formyl-3,9-dihydroxy-4,10-diprenylpterocarpan, by cristacarpin, and by erystagallin C
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additional information
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development of a rapid high-throughput screening method for PTP inhibitors, overview
-
additional information
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design, synthesis and evaluation of a series of bromo-retrochalcones as PTP1B inhibitors based on licochalcone A and E, overview
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additional information
not inhibited by H2O2 treatment
-
additional information
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not inhibited by H2O2 treatment
-
additional information
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not inhibited by camelliaolean A and camelliaolean B
-
additional information
structure-based drug design
-
additional information
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structure-based drug design
-
additional information
IPTG and lactose inhibit the sugar hydrolase activity of the enzyme PTPRdelta
-
additional information
IPTG and lactose inhibit the sugar hydrolase activity of the enzyme PTPRdelta
-
additional information
no autoinhibition
-
additional information
abietane-type diterpenoids inhibit protein tyrosine phosphatases by stabilizing an inactive enzyme conformation. Abietane-type diterpenoids, a biologically active class of phytometabolites with largely nonpolar structures, are used for the development of pharmaceutically relevant PTP inhibitors. Minor changes in the structures of abietane-type diterpenoids (e.g. the addition of hydrogens) can improve potency (i.e. lower IC50) by several fold. Trodusquemine and benzofuran derivatives bind to C-terminal allosteric sites that attenuate WPD loop dynamics. Mechanisms of inhibition, dynamic docking, modelling, overview
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additional information
design and synthesis of azolyl flavonoids as enzyme inhibitors of protein tyrosine phosphatase 1B, molecular modeling and dynamics studies, using the crystal structure of PTP1B (PDB ID 1G1H) reveals the selectivity of triazolyl flavonoid inhibitor 7-(2-(1H-1,2,4-triazol-1-yl)ethoxy)-2-phenyl-4H-chromen-4-one for PTP1B over the closely related T-cell protein tyrosine phosphatase (TCPTP), detailed overview. The inhibitory effects and kinetics analysis of the azoyl flavonoids against PTPs are measured, using 4-nitrophenol phosphate as the substrate
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additional information
the active sites of PTPs are exceptionally conserved and charged, making it nearly impossible to develop PTP inhibitors that are selective. But targeting PTP protein (substrate/regulatory) interaction sites, which are distal from the active sites, are highly viable and suitable drug targets. Domains outside PTP catalytic domains have also been demonstrated to directly alter PTP activity. Development of drugs that bind to intrinsically disordered regions of the enzyme, overview
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additional information
design of non-natural allosteric-inhibition sites in PTPs, in which a tricysteine moiety is engineered within the PTP catalytic domain at a conserved location outside of the active site. Introduction of the tricysteine motif, which does not exist in any wild-type PTP, serves to sensitize target PTPs to inhibition by a biarsenical compound, providing a generalizable strategy for the generation of allosterically sensitized (as) PTPs. Biarsenical reagents as enzyme inhibitors, overview. Enzyme asPTP catalytic domains have differing biarsenical sensitivities, with some being most potently inhibited by biarsenical compounds with large interarsenical distances, whereas others prefer compounds with relatively small interarsenical distances. AsCy3 is an optimized inhibitor of of engineered enzyme asPTP1B
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additional information
identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase, overview
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additional information
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identification of a benzo imidazole thiazole derivative as the specific irreversible inhibitor of protein tyrosine phosphatase, overview
-
additional information
wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes, determination and analysis of inhibitors isolated from aerial parts of Wedelia prostrata collected in Manado (Indonesia) and Wedelia chinensis collected on Iriomote Island (Okinawa, Japan). For inhibitory assays, 4-nitrophenyl phosphate is used as enzyme substrate
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additional information
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wedelolide derivatives and structure-activity relationships of protein tyrosine phosphatase 1B inhibitory ent-kaurene diterpenes, determination and analysis of inhibitors isolated from aerial parts of Wedelia prostrata collected in Manado (Indonesia) and Wedelia chinensis collected on Iriomote Island (Okinawa, Japan). For inhibitory assays, 4-nitrophenyl phosphate is used as enzyme substrate
-
additional information
4-[(5-arylidene-4-oxothiazolidin-3-yl)methyl]benzoic acid derivatives determined as active potent allosteric inhibitors of protein tyrosine phosphatase 1B, in silico studies and in vitro evaluation as insulinomimetic and anti-inflammatory agents, binding modes and inhibitory mechanism, docking studies, detailed overview
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additional information
phosphorylation of PTPN12 at Ser19 changes its substrate interface, and by doing so, selectively decreases its activity toward the human epidermal growth factor receptor 2 (HER2)-pY1196 site, but not other HER2 phosphorylation sites or other known PTPN12 substrates, such as SRC, paxillin, PAK1,VAV2, p130Cas, FAK, and p190RhoGAP
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additional information
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phosphorylation of PTPN12 at Ser19 changes its substrate interface, and by doing so, selectively decreases its activity toward the human epidermal growth factor receptor 2 (HER2)-pY1196 site, but not other HER2 phosphorylation sites or other known PTPN12 substrates, such as SRC, paxillin, PAK1,VAV2, p130Cas, FAK, and p190RhoGAP
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additional information
inhibition of protein tyrosine phosphatase-1B by vanadyl (VO2+) chelates, competitive and noncompetitive inhibition modes, overview
-
additional information
chemical library screening, kinetic and computational studies of mixed-type inhibitors of protein tyrosine phosphatase 1B, docking and molecular dynamic simulations studies, and enzyme interaction analysis, overview. For the inhibition assays, 4-nitrophenyl phosphate is used as enzyme substrate
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additional information
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unaffected by EDTA
-
additional information
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EDTA, sodium tartrate, sodium fluoride, or okadaic acid have no effect on activity
-
additional information
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inhibition of PTP-PEST by RNAi reduces formation of podosomal structures at the cell periphery and reduces bone resorption indicating a positive functional role for this PTP in promoting osteoclast activity
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additional information
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beta2AR stimulation on a B cell phosphorylates and inactivates HePTP in a Gs/cAMP/PKA-dependent manner
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additional information
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interaction between the alpha-cytoplasmic tail of a1beta1 integrin and TCPTP activates TCPTP by disrupting an inhibitory intramolecular bond in TCPTP, screening of screened 64280 small molecules for TCPTP inhibition, overview
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additional information
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not inhibitory: okadaic acid
-
additional information
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synthesis and inhibitory activity of 38 synthetic chalcones towards PtpA, the predominant factor for the activity is the molecule planarity/hydrophobicity and the nature of the substituents, structure-activity analysis, overview. No inhibition by 3a, 3b, 3c, 4h, 5l, 6d, 6g, and 6j
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additional information
inhibitor synthesis, structure-activity relationships, overview
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additional information
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inhibitor synthesis, structure-activity relationships, overview
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additional information
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PTP bidentate inhibitor library synthesis and screening, overview. The bidentate inhibitors have three components: 1. the warheads, alkyne-containing N-phenyloxamic acids that are cell-permeable, potent bioisosteric phosphotyrosine mimics, 2. a variety of different types of building blocks that act as the secondary-site binders, and 3. azide-containing linkers of different lengths joining the warhead and the building blocks, overview
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additional information
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design of structure based cyclic peptide inhibitors, synthesis involves a crucial intramolecular transamidation via a ring opening reaction. All the compounds show moderate to good inhibitory activities against MPtpA in micromolar concentrations, enzyme docking study, overview
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additional information
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unaffected by EDTA
-
additional information
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in absence of externally added Ca2+, no effect of ethylene glycol bis(2-amino-ethylether) N,N,NĀ,NĀ-tetracetic acid or trifluoperazine. Not inhibitory: okadaic acid
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additional information
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inhibitor docking studies with PTP-1B, overview
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additional information
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inhibitor design using the crystal structure of PtpA, overview
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additional information
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unaffected by okadaic acid
-
additional information
Q6JHV2
not inhibitory: pentamidine, okadaic acid, sodium fluoride up to 5 mM, EDTA up to 10 mM
-
additional information
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not inhibitory: pentamidine, okadaic acid, sodium fluoride up to 5 mM, EDTA up to 10 mM
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additional information
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overview, development of inhibitors
-
additional information
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the inhibition mechanism of [RuIII(EDTA)(OH2/OH)]1-/2- shows similar interactions, that may be important in the anti-cancer properties of the active forms of many Ru pro-drugs
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additional information
Yersinia enterolytica
-
inhibitory potency of gold(I) complexes containing N-heterocyclic carbene ligands versus cysteine-dependent protein tyrosine phosphatases, reversible inhibhition, overview
-
additional information
shows no sensitivity to H2O2
-
additional information
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shows no sensitivity to H2O2
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