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(1R,2R)-2-[4'-[(phenylcarbamoyl)amino][1,1'-biphenyl]-4-carbonyl]cyclopentane-1-carboxylic acid
-
(2alpha,3beta)-2,3-dihydroxyurs-12-en-28-oic acid
-
IC50: 0.0443 mM
(2E)-1-[2,4-dihydroxy-6-methoxy-3-[(2R)-5-methyl-2-(1-methylethenyl)hex-4-en-1-yl]phenyl]-3-(2,4-dihydroxyphenyl)prop-2-en-1-one
-
IC50: 0.0098 mM
(2E,4Z,8E)-N-[9-(3,4-methylenedioxyphenyl)-2,4,8-nonatrienoyl]piperidine
-
IC50: 0.0298 mM, isolated from the extracts of fruits of Piper longum and Piper nigrum
(2R,3R)-2-(2,4-Dihydroxy-phenyl)-3,7-dihydroxy-8-((R)-5-hydroxy-2-isopropenyl-5-methyl-hexyl)-5-methoxy-chroman-4-one
-
i.e. kushenol H, prenylflavonoid from Sophora flavescens, 50% inhibition at 0.142 mM
(2R,3S)-2-(2,4-Dihydroxy-phenyl)-3,7-dihydroxy-8-((R)-5-hydroxy-2-isopropenyl-5-methyl-hexyl)-5-methoxy-chroman-4-one
-
i.e. kushenol K, prenylflavonoid from Sophora flavescens, 50% inhibition at 0.250 mM
(2S)-1-(3-[[(2S)-1-ethoxy-4-phenylbutan-2-yl]sulfamoyl]anilino)-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
-
-
(2S)-1-[(1-[[(1S)-1-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-3-phenylpropyl]carbamoyl]cyclopentyl)amino]-4-methyl-1-oxopentan-2-yl 2,2-dimethylpropanoate
-
-
(4-[4-[4-(2-amino-5-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4-[4-[4-(5-chloro-2-nitrobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4-[4-[4-([[2-fluoro-5-(trifluoromethyl)phenyl]carbamoyl]amino)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)acetic acid
-
(4S,7R)-4-(5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)-2,2-dimethyl-4,7-bis[(4E)-4-methyl-5-[(2R)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-1-yl]-4,5,6,7-tetrahydro-1-benzofuran-3(2H)-one
89.23% inhibition
(trans-4-(4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-(4-[(5-cyclopentylethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
-
(trans-4-(4-[(5-cyclopentylmethyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
-
(trans-4-(4-[(5-[1-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-(4-[(5-[2-chlorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-(4-[(5-[2-fluorobenzyl]-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl)cyclohexyl)acetic acid
-
inhibitor displays good metabolic stability and high intestinal permeability values
(trans-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
-
-
(trans-4-[4-[(5-benzyl-1,2,4-oxadiazol-3-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
-
-
(trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenyl]cyclohexyl)acetic acid
-
-
1,2-diacyl-sn-glycerol
-
dicaprin, dimyristin, dipalmitin, high concentration
1-acyl-sn-glycero-3-phosphocholine
-
activation, at low concentrations, inhibition above 0.2 mM
1-O-Hexadecyl-2-oleoyl-sn-glycerol
-
competitive
1-O-Hexadecylpropanediol-3-phosphocholine
-
activation, low concentration, inhibitory at high concentration
1-[2,4-dihydroxy-3-(2-isopropenyl-5-methyl-hex-4-enyl)-6-methoxy-phenyl]-3-(2,4-dihydroxy-phenyl)-propenone
-
i.e. kuraridin, prenylflavonoid from Sophora flavescens, 50% inhibition at 0.099 mM
2-(2,4-dihydroxy-phenyl)-7-hydroxy-8-(2-isopropenyl-5-methyl-hex-4-enyl)-5-methoxy-chroman-4-one
-
i.e. kurarinone, prenylflavonoid from Sophora flavescens, 50% inhibition at 0.0109 mM
2-(2,4-dihydroxy-phenyl)-7-hydroxy-8-[2-(3-hydroxy-3-methyl-butyl)-3-methyl-but-3-enyl]-5-methoxy-chroman-4-one
-
i.e. kurarinol, prenylflavonoid from Sophora flavescens, 50% inhibition at 0.0086 mM
3,5-dimethyl-6-([(6E)-6-methyl-7-[(2S)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]hept-6-en-1-yl]oxy)pyrazine-2-carboxamide
-
3-(4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexyl)propanoic acid
-
3-oxoolean-12-en-27-oic acid
-
the compound exhibits strong inhibition efficacy towards diacylglycerol acyltransferases 1 and 2, and acts competitively against oleoyl-CoA in vitro
3alpha-hydroxyolean-12-en-27-oic acid
-
-
3beta-hydroxyolean-12-en-27-oic acid
-
-
4-amino-6-[(4E)-4-methyl-5-[(2R)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-2-yn-1-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one
-
4-amino-6-[(4E)-4-methyl-5-[(2S)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]pent-4-en-2-yn-1-yl]-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5(6H)-one
-
4-[(4-chloro-3-fluorophenyl)methyl]-N-[2-(3,4-diethoxyphenyl)ethyl]-4H-thieno[3,2-b]pyrrole-5-carboxamide
-
EC value is 0.000009 mM
4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)piperidine-1-carbonyl]cyclohexane-1-carboxylic acid
-
4-[4-[4-(3-chlorobenzamido)phenyl]thieno[3,2-d]pyrimidin-7-yl]cyclohexane-1-carboxylic acid
-
5,5'-dithio-bis(2-nitrobenzoic acid)
6,8-diprenylgenistein
-
IC50: 0.0067 mg/ml
7beta-(3-ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
8-angeloyloxy-3,4-epoxy-bisabola-7(14),10-dien-2-one
8-prenylleutone
-
IC50: 0.015 mg/ml
aceriphyllic acid A
-
the compound exhibits strong inhibition efficacy towards diacylglycerol acyltransferases 1 and 2, and acts competitively against oleoyl-CoA in vitro
alpinumisoflavone
-
23% inhibition at 0.0125 mg/ml
ATP
-
ATP-dependent activity reduces activity in vitro by 30-40%
auriculatin
-
IC50: 0.0072 mg/ml
brachynereolide
-
IC50: 0.25 mM, above
cetyltrimethylammonium bromide
-
-
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
-
cis-4-(4-[[5-(cyclopentylamino)-1,3,4-thiadiazol-2-yl]carbamoyl]phenoxy)cyclohexane-1-carboxylic acid
-
-
cis-4-([5-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]pyridin-2-yl]oxy)cyclohexane-1-carboxylic acid
-
-
cis-4-[4-([3-[(3,5-difluorophenyl)methyl]-1,2,4-oxadiazol-5-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-[(3-benzyl-1,2,4-oxadiazol-5-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-[(5-anilino-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
cis-4-[[5-([5-[(3-chlorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)pyridin-2-yl]oxy]cyclohexane-1-carboxylic acid
-
-
crepidiaside C
-
IC50: 0.25 mM, above
cryptotanshinone
-
IC50: 0.0273 mM
dehydropipernonaline
-
noncompetitive inhibition, IC50: 0.0212 mM, isolated from the extracts of fruits of Piper longum and Piper nigrum
derrone
-
IC50: 0.0151 mg/ml
erysenegalensein D
-
IC50: 0.0015 mg/ml
erysenegalensein N
-
28% inhibition at 0.0125 mg/ml
erysenegalensein O
-
IC50: 0.0011 mg/ml
ethanol
-
43% inhibition when 0.04 ml are added to reaction mixture
ethyl 1-(1-[[(2-chlorophenyl)carbamoyl]amino]cyclohexane-1-carbonyl)piperidine-4-carboxylate
-
EC value is 0.0015 mM
ethyl 1-[N-[(2,4-dichlorophenyl)carbamoyl]-2-methylalanyl]piperidine-4-carboxylate
-
EC value is 0.00025 mM
germanicol acetate
-
IC50: 0.25 mM, above
HgCl2
-
90% at 0.03-0.05 mM, reversible by DTT
I-
-
substantial inhibition
iodoacetamide
-
15% inhibition at 1 mM, DTT protects
ixerin Y
-
IC50: 0.25 mM, above
KCl
-
500 mM, inhibits purified enzyme
lysophosphatidylcholine
-
activation at low concentrations, optimum at 0.075 mM, inhibitory above 0.2 mM
methyl 1-benzyl-3-[(furan-3-carbonyl)amino]-5-[(2-methylbutyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 1-benzyl-3-[(furan-3-carbonyl)amino]-5-[[(thiophen-3-yl)methyl]amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohex-3-en-1-yl)acetate
-
methyl 2-(4-(4-(4-((tert-butoxycarbonyl)amino)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl) acetate
-
methyl 2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
methyl 2-(4-(4-(4-aminophenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
methyl 3-benzamido-1-[(furan-2-yl)methyl]-5-[(2-methylbutyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 3-[(furan-2-carbonyl)amino]-1-(3-methylbutyl)-5-[(pentan-3-yl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 3-[(furan-3-carbonyl)amino]-1-(2-methylpropyl)-5-[(pentan-3-yl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 5-[(2,3-dihydro-1H-inden-2-yl)amino]-3-[(furan-3-carbonyl)amino]-1-(2-methylpropyl)-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 5-[[(4-acetamidophenyl)methyl]amino]-1-benzyl-3-[(furan-3-carbonyl)amino]-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl 5-[[(furan-3-yl)methyl]amino]-1-(2-methylpropyl)-3-(2-phenylacetamido)-1H-pyrrolo[2,3-b]pyridine-2-carboxylate
-
-
methyl cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
methyl trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
methyl ursolate
-
IC50: 0.0264 mM
Mn2+
-
73% inhibition at 2.5 mM
N-(1-[[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]amino]-2-methyl-1-oxopropan-2-yl)-4-fluorobenzamide
-
-
N-(4,5-dihydronaphtho[1,2-d]thiazol-2-yl)-2-(3,4-dimethoxy phenyl)acetamide
selective inhibitor of isoform DGAT2 when used at low concentrations; selective inhibitor of isoform DGAT2 when used at low concentrations
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-carbamoylcyclohexyl)benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(dimethylamino)ethyl]carbamoyl]cyclohexyl)benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-(trans-4-[[2-(morpholin-4-yl)ethyl]carbamoyl]cyclohexyl)benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2,3-dihydroxypropyl)carbamoyl]cyclohexyl]benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-hydroxy-2-methylpropyl)carbamoyl]cyclohexyl]benzamide
-
-
N-(5-benzyl-1,3,4-thiadiazol-2-yl)-4-[trans-4-[(2-methoxyethyl)carbamoyl]cyclohexyl]benzamide
-
-
n-octyl-beta-D-glucopyranoside
-
weak
N-[(2S)-1-ethoxy-4-phenylbutan-2-yl]-1-[2-(tricyclo[3.3.1.1~3,7~]decan-2-yl)acetamido]cyclopentane-1-carboxamide
-
-
N-[1,5-bis(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
N-[1-(3,5-dimethylphenyl)-4,5,6,7-tetrahydro-1H-indazol-4-yl]-1,2,3-thiadiazole-4-carboxamide
-
EC value is 0.10 mM
N-[1-(4-fluoro-2-methylphenyl)-5-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
N-[1-(4-fluorophenyl)-5-[2-(4-fluorophenyl)propan-2-yl]-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
N-[1-(4-hydroxyphenyl)-4,5,6,7-tetrahydro-1H-indazol-4-yl]pyridine-2-carboxamide
-
EC value is 0.00000034 mM
N-[2-(3,4-diethoxyphenyl)ethyl]-4-methyl-4H-thieno[3,2-b]pyrrole-5-carboxamide
-
EC value is 0.011 mM
N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-(1-methylcyclopropane-1-carbonyl)alaninamide
-
-
N-[5-tert-butyl-1-(4-fluorophenyl)-1H-1,2,4-triazol-3-yl]-2-methyl-N~2~-[1-(trifluoromethyl)cyclopropane-1-carbonyl]alaninamide
-
-
oleate
-
noncompetitive inhibition, IC50: 0.0545 mM
p-chloromercuribenzene sulfonate
-
complete inhibition, DTT protects
p-chloromercuribenzoate
-
complete inhibition, DTT protects
palmitoyl-CoA
-
high concentration
phenylpyropene C
-
noncompetitive
phosphatidylethanolamine
-
-
pipernonaline
-
IC50: 0.0372 mM, isolated from the extracts of fruits of Piper longum and Piper nigrum
piperrolein B
-
IC50: 0.0201 mM, isolated from the extracts of fruits of Piper longum and Piper nigrum
retrofractamide C
-
IC50: 0.9 mM, above, isolated from the extracts of fruits of Piper longum and Piper nigrum
sesquiterpenoids
-
weak inhibition
-
Soybean trypsin inhibitor
-
-
Tergitol NP-40
-
microsomal preparation
tert-butyl (2S)-2-[[1-([(2S)-2-[(2,2-dimethylpropanoyl)oxy]-4-methylpentanoyl]amino)cyclopentane-1-carbonyl]amino]-4-phenylbutanoate
-
-
tert-butyl (4-(7-bromothieno[3,2-d]pyrimidin-4-yl)phenyl)carbamate
-
trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
trans-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetic acid
-
trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenoxy]cyclohexane-1-carboxylic acid
-
-
trans-4-[4-[(5-benzyl-1,3,4-thiadiazol-2-yl)carbamoyl]phenoxy]cyclohexane-1-carboxylic acid
-
-
Trifluoperazine
-
0.5 mM, in the presence of suboptimal phosphatidic acid concentration
[(1r,4r)-4-(4-[[5-(3,4-difluoroanilino)-1,3,4-oxadiazole-2-carbonyl]amino]phenyl)cyclohexyl]acetic acid
-
[(1r,4r)-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl]acetic acid
-
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
[(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid
89.32% inhibition
[4-(4-[4-[(naphthalene-2-carbonyl)amino]phenyl]thieno[3,2-d]pyrimidin-7-yl)cyclohexyl]acetic acid
-
[4-[4-(4-[[(3-chlorophenyl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[4-[4-(4-[[(4-chloropyridin-2-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[4-[4-(4-[[(5-bromopyridin-3-yl)carbamoyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[4-[4-(4-[[2-phenyl-5-(trifluoromethyl)-1,3-oxazole-4-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[4-[4-(4-[[6-(trifluoromethyl)pyridine-3-carbonyl]amino]phenyl)thieno[3,2-d]pyrimidin-7-yl]cyclohexyl]acetic acid
-
[trans-4-(4-[[5-(2-cyclopentylethyl)-1,3,4-thiadiazol-2-yl]carbamoyl]phenyl)cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(3,5-difluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-oxadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(4-fluorophenyl)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[(cyclopentyloxy)methyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[2-(oxolan-2-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
[trans-4-[4-([5-[2-(oxolan-3-yl)ethyl]-1,3,4-thiadiazol-2-yl]carbamoyl)phenyl]cyclohexyl]acetic acid
-
-
2-Bromooctanoate
-
50% inhibition at 1.5 mM
2-Bromooctanoate
-
specific inhibition
2-Bromooctanoate
-
specific inhibition
5,5'-dithio-bis(2-nitrobenzoic acid)
-
i.e. DTNB, complete inhibition, DTT protects
5,5'-dithio-bis(2-nitrobenzoic acid)
-
11% inhibition at 1 mM
7beta-(3-ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
-
-
7beta-(3-ethyl-cis-crotonoyloxy)-1alpha-(2-methylbutyryloxy)-3,14-dehydro-Z-notonipetranone
-
-
8-angeloyloxy-3,4-epoxy-bisabola-7(14),10-dien-2-one
-
-
8-angeloyloxy-3,4-epoxy-bisabola-7(14),10-dien-2-one
-
-
acyl-CoA
substrate inhibition is observed at higher concentrations of acyl-CoA
acyl-CoA
substrate inhibition of DGAT1, acyl-CoA binding protein AtACBP6 from Arabidopsis thaliana slightly enhances the substrate inhibition of DGAT1 at the acyl-CoA concentrations above 0.01 mM
acyl-CoA
-
C-10-CoA to C-16-CoA, high concentration
betulinic acid
-
a lupane-type triterpenoid, isolated from methanolic extracts of Alnus hirsuta, inhibition of Hep-G2 cell triacyglycerol biosynthesis
betulinic acid
-
a lupane-type triterpenoid, isolated from methanolic extracts of Alnus hirsuta, noncompetitive inhibition, IC50: 0.0096 mM
bovine serum albumin
-
binds palmitoyl-CoA and decreases activity towards palmitoyl-CoA, but not butyryl-CoA
-
bovine serum albumin
-
strong inhibition
-
bovine serum albumin
-
activation at 0.1%, inhibition at 2.5%
-
Ca2+
-
-
Ca2+
-
48% inhibition at 2.5 mM
CaCl2
5 mM, 30% inhibition
CaCl2
-
2 mM, inhibits purified enzyme but not activity in lipid body fraction
CHAPS
-
-
cholate
-
-
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
E2RDN4
-
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
cis-2-(4-(4-(4-(3-(3-chlorophenyl)ureido)phenyl)thieno[3,2-d]pyrimidin-7-yl)cyclohexyl)acetate
-
CoA
above 50 mM, about 70% inhibition above 300 mM
CoA
noncompetitively inhibits isozyme BnaC.DGAT1.a. The N-terminal domain of isoform BnaA.DGAT1.b can interact with acyl-CoA at a possible allosteric site, and CoA can displace the thioester
CoA
an allosteric modulator of DGAT1, interaction with the cytoplasmic N-terminal region, overview
deoxycholate
-
-
DTT
-
above 2 mM
DTT
-
microsomal preparation
kuraridin
-
IC50: 0.0098 mM
kurarinone
-
-
kurarinone
-
IC50: 0.0048 mg/ml
Mg2+
-
-
Mg2+
-
10% inhibition at 2.5 mM, 40% at 8.0 mM
MgCl2
5 mM, 17% inhibition
MgCl2
-
5 mM, inhibits purified enzyme but not activity in lipid body fraction
MnCl2
5 mM, 30% inhibition
N-ethylmaleimide
-
95% loss of activity after preincubation with 40 mM
N-ethylmaleimide
-
inhibits solubilized enzyme, but not membrane-bound enzyme
niacin
-
30% inhibition
niacin
a specific noncompetitive DGAT2 inhibitor. Dga1p enzyme mutant versions exhibit DGAT2 specific activity, which is inhibited by niacin. The decrease is 70% for Dga1pDELTA19 and up to 99.5% for Dga1pDELTA85
oleanolic acid
-
-
oleanolic acid
-
IC50: 0.0317 mM
oleoyl-CoA
substrate inhibition
oleoyl-CoA
BnaDGAT1 exhibits a sigmoidal response and eventual substrate inhibition with respect to increasing concentrations of oleoyl-CoA. In the presence of phosphatidic acid (PA), the oleoyl-CoA saturation plot becomes more hyperbolic and desensitized to substrate inhibition. BnaDGAT1 is less susceptible to substrate inhibition at 0.005-0.020 mM oleoyl-CoA in the presence of 1 mg/ml BSA
oleoyl-CoA
an allosteric modulator of DGAT1, interaction with the cytoplasmic N-terminal region, overview
oleoyl-CoA
substrate inhibition
oleoyl-CoA
-
substrate inhibition
oleoyl-CoA
substrate inhibition; substrate inhibition
sodiumdodecyl sulfate
-
-
sodiumdodecyl sulfate
-
-
sodiumdodecyl sulfate
-
irreversible denaturation
Triton X-100
-
microsomal preparation
Triton X-100
-
50% inhibition at 0.1-0.2%
Triton X-100
-
above 0.05 mM
Triton X-100
-
microsomal preparation
tussilagone
-
-
tussilagonone
-
-
Tween 20
-
-
Tween 20
-
99% inhibition at 5 mg/ml, 89% inhibition at 1 mg/ml, 49% inhibition at 0.5 mg/ml
XP620
-
dihydrothiopyrancarboxamide
XP620
-
dihydrothiopyrancarboxamide
XP620
-
dihydrothiopyrancarboxamide
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
E2RDN4
-
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
[(1r,4r)-4-[4-(5-[[6-(trifluoromethyl)pyridin-3-yl]amino]pyridin-2-yl)phenyl]cyclohexyl]acetic acid
-
additional information
the intrinsically disordered region (IDR) of the N-terminal domain encompasses an autoinhibitory motif. Purified BnaDGAT1 can be phosphorylated and inactivated by SnRK1
-
additional information
the intrinsically disordered region (IDR) of the N-terminal domain encompasses an autoinhibitory motif. Purified BnaDGAT1 can be phosphorylated and inactivated by SnRK1
-
additional information
the intrinsically disordered region (IDR) of the N-terminal domain encompasses an autoinhibitory motif. Purified BnaDGAT1 can be phosphorylated and inactivated by SnRK1
-
additional information
phosphorylation downregulates the activity of the enzyme
-
additional information
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phosphorylation downregulates the activity of the enzyme
-
additional information
the highly disordered segment at the enzyme's N-terminus is involved in the downregulation of DGAT1 activity, suggesting the presence of an autoinhibitory motif
-
additional information
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the highly disordered segment at the enzyme's N-terminus is involved in the downregulation of DGAT1 activity, suggesting the presence of an autoinhibitory motif
-
additional information
the cytoplasmic N-terminal domain of Brassica napus diacylglycerol acyltransferase, (DGAT1) includes an inhibitory module and allosteric binding sites, conformational heterogeneity in the N-terminal domain of DGAT1
-
additional information
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the cytoplasmic N-terminal domain of Brassica napus diacylglycerol acyltransferase, (DGAT1) includes an inhibitory module and allosteric binding sites, conformational heterogeneity in the N-terminal domain of DGAT1
-
additional information
E2RDN4
in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview
-
additional information
-
in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview
-
additional information
-
no inhibition by Ca2+
-
additional information
design and synthesis of diacylglycerol acyltransferase 1 inhibitors based on aphadilactone C. The lactone group of aphadilactone C is introduced into the [(1r,4r)-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl]acetic acid and [(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid (which have entered into clinical research) to verify whether the lactone in aphadilactone C plays the same role as carboxylic group in [(1r,4r)-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl]acetic acid and [(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid. The final in vitro assay shows that the synthesized compounds have not the inhibition activity to DGAT1. This might suggest that the inhibition mechanism of aphadilactone C is not the same as of [(1r,4r)-4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexyl]acetic acid and [(1r,4r)-4-[4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl]cyclohexyl]acetic acid. No inhibition by 3,5-dimethyl-6-[(1E)-1-[(2S)-4-methyl-6-oxo-3,6-dihydro-2H-pyran-2-yl]prop-1-en-2-yl]pyrazine-2-carboxamide
-
additional information
-
high-throughput screening for enzyme inhibitors, quantitative-high throughput image-based assay, overview. The activity of the identified lipid storage inhibitors is evolutionary conserved. Three scaffolds: structures are characterized by a tetrahydroindazole (CT1), thienopyrrole (CT2) or arylureido (CT3) core, phenotypic analysis of thienopyrrole (CT2) treated cells
-
additional information
a series of thieno[3,2-d]pyrimidine derivatives are synthesized and their inhibitory effects against diacylglycerol acyltransferase 1 (DGAT-1) are assessed
-
additional information
in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview
-
additional information
-
in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview
-
additional information
no inhibition by selective DGAT1 inhibitor PF-04620110
-
additional information
-
no inhibition by selective DGAT1 inhibitor PF-04620110
-
additional information
DGAT2 inhibitor alone has very modest effect but inhibition of both isoforms substantially reduced 13C fatty acid incorporation into triglyceride (TG) pool in the heart. Coinhibition of DGAT1/2 in the heart abrogates TG turnover and protects the heart against high fat diet-induced lipid accumulation with no adverse effects on basal or dobutamine-stimulated cardiac function. A DGAT2 inhibitor does not further change substrate oxidation in DGAT1 iKO mice
-
additional information
DGAT2 inhibitor alone has very modest effect but inhibition of both isoforms substantially reduced 13C fatty acid incorporation into triglyceride (TG) pool in the heart. Coinhibition of DGAT1/2 in the heart abrogates TG turnover and protects the heart against high fat diet-induced lipid accumulation with no adverse effects on basal or dobutamine-stimulated cardiac function. A DGAT2 inhibitor does not further change substrate oxidation in DGAT1 iKO mice
-
additional information
-
DGAT2 inhibitor alone has very modest effect but inhibition of both isoforms substantially reduced 13C fatty acid incorporation into triglyceride (TG) pool in the heart. Coinhibition of DGAT1/2 in the heart abrogates TG turnover and protects the heart against high fat diet-induced lipid accumulation with no adverse effects on basal or dobutamine-stimulated cardiac function. A DGAT2 inhibitor does not further change substrate oxidation in DGAT1 iKO mice
-
additional information
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diethyl-p-nitrophenylphosphate, diisopropyl fluorophosphate
-
additional information
-
10% v/v acetone, sn-2-monoolein
-
additional information
-
not inhibitory: hesperetin, naringenin, quercetin, kaempferol up to 0.8 mM
-
additional information
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an ethylacetic extract of Youngia koidzumiana, a plant endemic to the Mount Chiri region of Korea, significantly inhibits the liver microsome enzyme
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additional information
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inhibition mechanism, the inhibitory activity of Piper fruits is influenced by the presence of the piperidine group rather than by isobutyl group, overview
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additional information
in vivo inhibitory activity thieno[3,2-d]pyrimidine derivatives against diacylglycerol acyltransferase 1 (DGAT-1) and effects on microsomes and cytochrome P-450, overview
-