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(1Z)-2-{[3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl}ethanehydrazonic acid
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(2-tert-butoxy-2-oxoethyl)(dimethyl)sulfonium
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(2-[[(1R)-3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-1-carboxy-3-oxopropyl]amino]-2-oxoethyl)(dimethyl)sulfanium bromide
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(2-[[4-(methoxycarbonyl)benzyl]oxy]-2-oxoethyl)(dimethyl)sulfonium
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(2-[[6-(methoxycarbonyl)naphthalen-2-yl]methoxy]-2-oxoethyl)(dimethyl)sulfonium
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(2E)-3-(4-nitrophenyl)-1-(pyridin-3-yl)prop-2-en-1-one
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reversible, competitive with the acyl donor substrate
(2S)-2-[[(benzyloxy)carbonyl]amino]-4-[(prop-2-enoyl)amino]butanoic acid
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(2-hydroxybenzamido)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(3-hydroxybenzamido)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(4-hydroxybenzamido)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(nicotinamido)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(prop-2-yn-1-yloxy)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(pyrazine-2-carboxamido)-pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-fluoropyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-hydroxypyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-methoxypyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-phenylpyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 4-(benzyloxy)-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 4-amino-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 4-benzamido-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(2S,4R)-quinolin-3-ylmethyl 4-benzyl-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(2-hydroxyphenyl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(3-chlorophenyl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(3-hydroxyphenyl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(4-chlorophenyl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(4-hydroxyphenyl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(5-fluoro-1H-indol-3-yl)pyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-fluoropyrrolidine-1-carboxylate
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(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-phenylpyrrolidine-1-carboxylate
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(3E)-1-benzyl-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-3-(2-oxopropylidene)-6-(trifluoromethoxy)-1,3-dihydro-2H-indol-2-one
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(3E)-3-[2-(3-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
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(3E)-3-[2-(4-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
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(3E)-3-[2-(5-bromopyridin-3-yl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
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(3E)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-1-(2-methylpropyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-1-(cyclohexylmethyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-1-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-(2-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-(3-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-(3-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-(4-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-(4-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-(6-methoxypyridin-3-yl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-2-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(2-phenylethyl)-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(3-phenylpropyl)-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(propan-2-yl)-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-phenyl-1,3-dihydro-2H-indol-2-one
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(3E)-4-chloro-3-[2-oxo-2-(pyridin-4-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-5-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-5-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
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(3E)-5-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-5-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-5-nitro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-6-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-6-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-6-fluoro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
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(3E)-7-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(3E)-7-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
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(3E)-7-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
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(4R)-1-[(benzyloxy)carbonyl]-4-hydroxy-L-prolyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
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(5-bromothiophen-2-yl)(4-methyl-1H-pyrazol-1-yl)methanone
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(E)-1-(1-(2-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
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(E)-1-(1-(3-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
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(E)-1-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
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(E)-1-(1-(cyclohexylmethyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
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(E)-1-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
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(naphthalen-2-yl)methyl 4-(N-acryloylglycyl)piperazine-1-carboxylate
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(naphthalen-2-yl)methyl 4-[N-(bromoacetyl)glycyl]piperazine-1-carboxylate
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(R)-quinolin-3-ylmethyl 3-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-(1-methyl-1H-benzo[d]imidazol-2-yl)methyl 2-((((S)-3-bromo-4,5-dihydro-isoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-(1H-benzo[d]imidazol-2-yl)methyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-(R)-1-(naphthalen-2-yl)ethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-(R)-1-(quinolin-3-yl)ethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-(S)-1-(naphthalen-2-yl)ethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-2,3-dimethoxybenzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-3-(benzyloxy)benzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-3-fluorobenzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-4-ethynylbenzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-benzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)pyrrolidine-1-carboxylate
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(S)-N-(((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-2-(1-(dimethylamino)naphthalene-5-sulfonamido)-3-(1H-indol-3-yl)propanamide
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the majority of cellular TG2 cannot be inhibited in intact cells. The inhibitor potently inhibits cell lysate TG2 activity in the presence of calcium
(S)-N-(((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)pyrrolidine-2-carboxamide
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(S)-prop-2-yn-1-yl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-pyridin-2-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-pyridin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-pyridin-4-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)-4-phenyl-2,5-dihydro-1H-pyrrole-1-carboxylate
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(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-2-methylpyrrolidine-1-carboxylate
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(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)azetidine-1-carboxylate
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(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)piperidine-1-carboxylate
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(S)-quinolin-3-ylmethyl 2-(2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)amino)-2-oxoethyl)pyrrolidine-1-carboxylate
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(S)-quinolin-3-ylmethyl 3-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate
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(S)-quinolin-4-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-quinoxalin-2-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
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(S)-tert-butyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)pyrrolidine-1-carboxylate
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1,1'-methanediylbis(1H-indole-2,3-dione)
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1,1'-[(2,5-dimethylbenzene-1,4-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
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1,1'-[(4,6-dimethylbenzene-1,3-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
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1,3-dimethyl-2-[(2-oxopropyl)thio]-1H-imidazol-3-ium
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1,3-dimethyl-2-[(2-oxopropyl)thio]imidazolium
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pan-transglutaminase inhibition inhibits terminal differentiation of keratinocytes, leading to a hyperproliferative epidermis with parakeratosis and enhanced expression of involucrin and cytokeratins 6 and 16. Expression of the differentiation-associated cytokeratin, cytokeratin 10, is reduced. Basement membrane integrity is also lost as a result of transglutaminase inhibition
1-(((3R,5S)-5-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)-1-((quinolin-3-ylmethoxy)carbonyl)pyrrolidin-3-yl)-carbamoyl)cyclobutanecarboxylic acid
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1-(1-benzothiophen-2-yl)-3-[benzyl(tert-butyl)amino]propan-1-one
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1-(6-methylpyridin-2-yl)piperazine
1-(6-nitropyridin-3-yl)piperazine
1-(ethenylsulfonyl)tricyclo[3.3.1.13,7]decane
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1-(furan-2-yl)-3-[(2-hydroxyethyl)(propan-2-yl)amino]propan-1-one
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1-(tricyclo[3.3.1.13,7]dec-1-yl)prop-2-en-1-one
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1-acetyl-L-prolyl-6-imino-5-oxo-L-norleucyl-L-leucyl-L-prolyl-L-phenylalaninamide
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1-ethyl-3-(4-methoxyphenyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
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1-[(2E)-3-(4-nitrophenyl)prop-2-enoyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-1-ium-3-olate
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reversible, competitive with the acyl donor substrate
1-[(benzyloxy)carbonyl]-L-prolyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
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2,3-dibromonaphthoquinone
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0.015 mM, 41.5% inhibition
2-(tricyclo[3.3.1.13,7]dec-1-yl)ethyl prop-2-enoate
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2-([2-[(3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-2,3-dioxopropyl)amino]-2-oxoethyl]sulfanyl)-1,3,4,5-tetramethyl-1H-imidazol-3-ium bromide
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2-([3-(2-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0015 mM, standard format
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
2-([3-(2-methoxyphenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.00082 mM, standard format, at 0.00047 mM, full progress curve
2-([3-(3-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0018 mM, standard format
2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.00045 mM, full progress curve
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
2-([3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio)acetohydrazide
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2-([3-(3-fluorophenyl)-5-(2-hydroxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0008 mM, standard format, at 0.00025 mM, full progress curve
2-([3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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2-([3-(3-fluorophenyl)-5-(3-diethylaminopropoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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2-([3-(3-fluorophenyl)-5-(3-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0014 mM, standard format
2-([3-(3-fluorophenyl)-5-methyl-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0002 mM, full progress curve
2-([3-(3-fluorophenyl)-5-phenyl-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.00093 mM, standard format, at 0.00071 mM, full progress curve
2-([3-(3-fluorophenyl)-7-methyl-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.00053 mM, full progress curve
2-([3-(3-methoxyphenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0021 mM, standard format
2-([3-(4-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0005 mM, standard format, at 0.00016 mM, full progress curve
2-([3-(4-methoxyphenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0018 mM, standard format
2-([5-(4-fluorophenyl)-4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
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50% inhibition at 0.0008 mM, standard format, at 0.00029 mM, full progress curve
2-aminonaphthoquinone
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0.015 mM, 33.4% inhibition
2-bromo-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
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2-bromo-3-hydroxynaphthoquinone
-
0.015 mM, 35.4% inhibition
2-chloro-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
-
-
2-[(2-hydrazinoethyl)thio]-3,5-diphenylthieno[2,3-d]pyrimidin-4(3H)-one
-
i.e. LDN-27219, reversible, slow-binding inhibitor that binds at the enzymes GTP site or a site that regulates binding of GTP
2-[(3-amino-2-oxopropyl)thio]-3-(3-fluorophenyl)-5-phenylthieno[2,3-d]pyrimidin-4(3H)-one
-
50% inhibition at 0.0053 mM, standard format
2-[(3-benzyl-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
50% inhibition at 0.0012 mM, standard format, at 0.00048 mM, full progress curve
2-[(3-methyl-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
50% inhibition at 0.0023 mM, standard format
2-[(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]-N,N-dimethylacetamide
-
-
2-[(4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)amino]acetohydrazide
-
50% inhibition at 0.0037 mM, full progress curve
2-[(4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)oxy]acetohydrazide
-
50% inhibition at 0.0045 mM, standard format
2-[(4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
50% inhibition at 0.0008 mM, standard format, at 0.00025 mM, full progress curve
2-[(4-oxo-3-phenyl-3,4-dihydroquinazolin-2-yl)thio]acetohydrazide
-
-
2-[(4-oxo-3-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
-
2-[(4-oxo-5-phenyl-3-pyridin-3-yl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
50% inhibition at 0.002 mM, standard format
2-[(6-methyl-4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]acetohydrazide
-
50% inhibition at 0.0015 mM, standard format, at 0.00016 mM, full progress curve
2-[[3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide
-
-
2-[[3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide
-
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide
-
-
2-[[3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio]acetohydrazide
-
-
2-[[3-(3-fluorophenyl)-4-oxo-6-phenyl-3,4-dihydroquinazolin-2-yl]thio]acetohydrazide
-
-
2-[[5-benzyl-3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide
-
-
2-[[5-[2-[3-(diethylamino)propoxy]phenyl]-3-(3-fluorophenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl]acetohydrazide
-
-
3-(3-methyl-3H-diaziren-3-yl)-N-[4-[(1E)-3-oxo-3-(pyridin-3-yl)prop-1-en-1-yl]phenyl]propanamide
-
reversible inhibitor and photolabel. In labeling experiments, specific labeling of residue C230
3-(4-acryloylaminobenzenesulfonylamino)-(R)-pyrrolidine-1-carboxylic acid benzyl ester
-
3-(4-acryloylaminobenzenesulfonylamino)-(S)-pyrrolidine-1-carboxylic acid benzyl ester
-
3-iodo-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
3-[(2E)-3-(3-nitrophenyl)prop-2-enoyl]-1H-benzotriazol-3-ium-1-olate
-
reversible, competitive with the acyl donor substrate
3-[(6-methyl-4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio]propanohydrazide
-
50% inhibition at 0.0013 mM, standard format
3-[benzyl(ethyl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
-
-
3-[benzyl(propan-2-yl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
-
-
3-[benzyl(propan-2-yl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
-
-
3-[benzyl(tert-butyl)amino]-1-(4-nitrophenyl)propan-1-one
-
-
3-[benzyl(tert-butyl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
3-[benzyl(tert-butyl)amino]-1-(5-chlorothiophen-2-yl)propan-1-one
-
-
3-[benzyl(tert-butyl)amino]-1-(thiophen-2-yl)propan-1-one
-
-
3-[bis(2-hydroxyethyl)amino]-1-(furan-2-yl)propan-1-one
-
-
4-(2-acryloylaminopyrimidine-5-sulfonyl)piperazine-1-carboxylic acid benzyl ester
-
4-(2-acryloylaminopyrimidine-5-sulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(3-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid benzyl ester
-
4-(4-acryloylamino-2-chlorobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(4-acryloylamino-2-fluorobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(4-acryloylamino-2-methoxybenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(4-acryloylamino-2-methylbenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(4-acryloylamino-2-trifluoromethylbenzenesulfonyl)-piperazine-1-carboxylic acid benzyl ester
-
4-(4-acryloylamino-3-fluorobenzenesulfonyl)piperazine-1-carboxylic acid benzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-chlorobenzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-methylbenzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 2-trifluoromethylbenzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid 3,5-difluorobenzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid benzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid cyclopentyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid methyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-1-ylmethyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid naphthalen-2-ylmethyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid 2,3-difluorobenzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid 4-fluorobenzyl ester
-
4-(4-acryloylaminobenzenesulfonyl)piperazine-1-carboxylicacid ethyl ester
-
4-(4-acryloylaminobenzenesulfonyl)[1,4]diazepane-1-carboxylicacid benzyl ester
-
4-(4-acryloylaminobenzenesulfonylamino)piperidine-1-carboxylic acid benzyl ester
-
4-(4-but-2-enoylaminobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(4-cyanobenzenesulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-(6-acryloylaminopyridine-3-sulfonyl)piperazine-1-carboxylic acid benzyl ester
-
4-(6-acryloylaminopyridine-3-sulfonyl)piperazine-1-carboxylic acid tert-butyl ester
-
4-fluoro-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
4-fluoro-N-[(2S)-1-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
4-hydroxymercuribenzoate
-
99% inactivation
4-[(4-acryloylaminobenzenesulfonylamino)methyl]-piperidine-1-carboxylic acid benzyl ester
-
4-[4-(1-oxobut-2-ynylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(2-cyanoacetylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(2-ethoxycarbonylvinyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
-
4-[4-(2-fluoroacryloylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(2-methylacryloylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(2-methylbut-2-enoylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(2-oxopropionylamino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(3-(E)-chloroacryloylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(3-(Z)-chloroacryloylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(3-cyanomethylureido)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(3-diazo-2-oxopropyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
-
4-[4-(3-ethoxycarbonylallyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
-
4-[4-(4,4,4-trifluoro-3-methylbut-2-enoylamino)-benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(4,4,4-trifluorobut-2-enoylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(4-diazo-3-oxobutyl)benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
-
4-[4-(acryloylmethyl-amino)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(cyanomethylcarbamoyl)benzenesulfonyl]piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-(ethoxycarbonylmethylamino)benzenesulfonyl]-piperazine-1-carboxylic acid tert-butyl ester
-
4-[4-acryloylamino-3-(isobutylmethylamino)-benzenesulfonyl]piperazine-1-carboxylic acid benzyl ester
-
5,5'-dithiobis (2-nitrobenzoic acid)
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
5,5'-methanediylbis(1H-indole-2,3-dione)
-
-
5,5'-oxybis(1H-indole-2,3-dione)
-
-
5-(4-acryloylaminobenzenesulfonyl)-2,5-diazabicyclo-[2.2.1]heptane-2-carboxylic acid tert-butyl ester
-
5-(4-acryloylaminobenzenesulfonyl)hexahydropyrrolo[3,4-c]pyrrole-2-carboxylic acid benzyl ester
-
5-(biotinamido)pentylamine
-
-
5-biotinamido pentylamine
5BP, 5BP is widely used in chromogenic TG2 assays, based on the ability of streptavidin conjugates to recognize its biotin substituent with high specificity
5-hydroxynaphthoquinone
-
0.015 mM, 46.1% inhibition
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
6,6'-oxybis(1H-indole-2,3-dione)
-
-
6-diazo-5-oxo-L-norleucine
DON
Ac-P(6-diazo-5-oxo-L-norleucine)LPF-NH2
high-affinity irreversible inhibitor of TG2. The inhibitor stabilizes TG2 in an extended conformation that is dramatically different from earlier transglutaminase structures. The active site is exposed, revealing that catalysis takes place in a tunnel, bridged by two tryptophan residues that separate acyl-donor from acyl-acceptor and stabilize the tetrahedral reaction intermediates
acetonitrile
48% residual activity at 5% (v/v)
acrylonitrile
68 and 48% residual activity at 2.5 and 5.0 mM, respectively
alpha-difluoromethylornithine
-
2.6 mM, 50% inhibition of putrescine transfer to casein, suicide substrate, irreversible, competitive to putrescine or fibrinonectin
ammonium
a natural inhibitor of the enzyme, prevents cross-linking activity
AMP
-
weak inhibition of liver transglutaminase
benzyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate
-
-
benzyl 4-[3-(acryloylamino)-2-oxopropanoyl]piperazine-1-carboxylate
-
-
benzyl 4-[3-[(ethenylsulfonyl)amino]-2-oxopropanoyl]piperazine-1-carboxylate
-
-
benzyl [(1R)-2-[[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]amino]-1-(methylamino)-2-oxoethyl]carbamate
-
irreversible
benzyl [(2S)-1-(4-acetylpiperazin-1-yl)-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-(4-benzoylpiperazin-1-yl)-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-(morpholin-4-yl)-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-1-[4-(phenylacetyl)piperazin-1-yl]-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-1-[4-(phenylmethanesulfonyl)piperazin-1-yl]-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-1-[4-(propane-2-sulfonyl)piperazin-1-yl]-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-6-[(prop-2-enoyl)amino]-1-[4-(pyridine-2-carbonyl)piperazin-1-yl]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-6-[(prop-2-enoyl)amino]-1-[4-(pyridine-3-carbonyl)piperazin-1-yl]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-6-[(prop-2-enoyl)amino]-1-[4-(pyridine-4-carbonyl)piperazin-1-yl]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-oxo-6-[(prop-2-enoyl)amino]-1-[4-(thiophene-2-sulfonyl)piperazin-1-yl]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[(2-aminoethyl)[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[(3-aminopropyl)[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[(4-aminobutyl)[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(2-chlorophenyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(7-hydroxy-2-oxo-2H-1-benzopyran-3-carbonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
i.e. VA5
benzyl [(2S)-1-[4-(benzenesulfonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(cyclohexanesulfonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(ethanesulfonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(methanesulfonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(naphthalene-1-carbonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(naphthalene-1-sulfonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(naphthalene-2-carbonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-(naphthalene-2-sulfonyl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-1-oxo-5-[(prop-2-enoyl)amino]pentan-2-yl]carbamate
-
-
benzyl [(2S)-1-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]carbamate
-
-
benzyl [(9S)-19-[[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-3,10-dioxo-14,17-dioxa-4,11-diazanonadec-1-en-9-yl]carbamate
-
-
beta-mercaptoethanolamine
-
mechanism of inhibition, mercapto group significantly influences substrate behaviour
beta-selenoethanolamine
-
-
Boc-DON-Gln-Ile-Val-OMe
-
-
BOC-DON-QIV-OMe
-
0.1 mM and 1 mM for normal skin and keloid scar, respectively
Ce3+
-
not reversible by Ca2+
CP30a
reversible inhibitor
CP4d
reversible inhibitor
cystamine dihydrochloride
-
1 mM and 10 mM for normal skin and keloid scar, respectively
cysteamine
-
50% inhibition at 0.178 mM
cysteine
-
85% inhibition
diethyl dicarbonate
-
not without Ca2+
dimethyl[2-oxo-2-(tricyclo[3.3.1.13,7]dec-1-yl)ethyl]sulfonium
-
-
dimethyl[2-oxo-2-(tricyclo[3.3.1.13,7]dec-1-ylmethoxy)ethyl]sulfonium
-
-
dimethyl[2-oxo-2-[2-(tricyclo[3.3.1.13,7]dec-1-yl)ethoxy]ethyl]sulfonium
-
-
dithiothreitol
-
1.5 mM, 42% inhibition, 16.5 mM, 40% inhibition
DMF
90% residual activity at 2.5 and 5% (v/v)
ERW1069
-
i.e. ((S)-1-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)amino)-3-(5-fluoro-1H-indol-3-yl)-1-oxopropan-2-yl)carbamate
ethenesulfonic acid (4-bromophenyl)amide
-
ethyl [(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]acetate
-
-
fluorenylmethyl [4-[(1E)-3-(1H-benzotriazol-1-yl)-3-oxoprop-1-en-1-yl]phenyl]carbamate
-
reversible, competitive with the acyl donor substrate
Gd3+
-
not reversible by Ca2+
glucosamine
-
the TGase 2 inhibitor, might be an attractive novel target for treatment of malignant cancers
GMP
-
at low levels of Ca2
GSSG
-
reversible inactivation, activity can be restored by treatment with dithiothreitol
HgCl2
-
5 mM, 96% inhibition in the presence of 10 mM Ca2+
hydroxylamine
-
100 mM, complete inhibition
isatin
-
weak, reversible inhibitor
K+
-
1 mM, 41% inhibition
La3+
-
not reversible by Ca2+
Li+
-
10 mM, complete inhibition
lysine
-
1 mM, 43% inhibition of DEAE-unabsorbed transglutaminase, 90% inhibition of DEAE-absorbed transglutaminase
menadione
-
0.015 mM, 97% inhibition
methyl 3-([(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]methyl)benzoate
-
-
methyl 4-([(3E)-4-chloro-2-oxo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-2,3-dihydro-1H-indol-1-yl]methyl)benzoate
-
-
methyl 4-[(1E)-3-(1H-benzotriazol-1-yl)-3-oxoprop-1-en-1-yl]benzoate
-
reversible, competitive with the acyl donor substrate
methyl 4-[(acryloyloxy)methyl]benzoate
-
-
methyl 4-[[(bromoacetyl)oxy]methyl]benzoate
-
-
methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
methyl 6-[(acryloyloxy)methyl]naphthalene-2-carboxylate
-
-
methyl 6-[[(bromoacetyl)oxy]methyl]naphthalene-2-carboxylate
-
-
methyl 6-[[(chloroacetyl)oxy]methyl]naphthalene-2-carboxylate
-
-
methyl N-[(benzyloxy)carbonyl]-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucinate bromide
-
-
methyl N2-[(benzyloxy)carbonyl]-N6-(prop-2-enoyl)-L-lysylglycinate
-
-
MgCl2
-
5 mM, 88% inhibition, 30% inhibition in the presence of 10 mM Ca2+
Monoiodoacetic acid
Nemipterus sp.
-
-
N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
N-(2-aminoethyl)-5-(dimethylamino)naphthalene-1-sulfonamide
-
-
N-(2-bromophenyl)acrylamide
-
N-(2-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-2-oxoethyl)prop-2-enamide
-
-
N-(3-aminopropyl)-5-(dimethylamino)naphthalene-1-sulfonamide
-
-
N-(3-bromophenyl)acrylamide
-
N-(3-methyl-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-glutaminylglycine
-
irreversible, ratio kinact to Ki 0.33 micromol per min
N-(4-aminobutyl)-5-(dimethylamino)naphthalene-1-sulfonamide
-
-
N-(4-bromobenzyl)acrylamide
-
N-(4-bromophenyl)acrylamide
-
N-(4-bromophenyl)propionamide
-
N-(4-fluorophenyl)acrylamide
-
N-(4-[4-[2-(2-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide
-
N-(4-[4-[2-(3-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide
-
N-(4-[4-[2-(4-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]- phenyl)acrylamide
-
N-(4-[4-[2-(4-phenoxyphenyl)acetyl]piperazine-1-sulfonyl]-phenyl)acrylamide
-
N-(phenylcarbonyl)-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-(tert-butoxycarbonyl)-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-acetyl-P(6-diazo-5-oxo-L-norleucine)LPF-NH2
-
active-site inhibitor
N-benzyloxycarbonyl-L-glutaminyl-6-(dimethylsulfonio)-5-oxo-L-norleucine
-
pan-transglutaminase inhibition inhibits terminal differentiation of keratinocytes, leading to a hyperproliferative epidermis with parakeratosis and enhanced expression of involucrin and cytokeratins 6 and 16. Expression of the differentiation-associated cytokeratin, cytokeratin 10, is reduced. Basement membrane integrity is also lost as a result of transglutaminase inhibition
N-carbobenzyloxy-L-phenylalanine 2-(acrylamido)ethylamide
-
-
N-carbobenzyloxy-L-phenylalanine 4-(acrylamido)butylamide
-
-
N-carbobenzyloxy-L-phenylalanine 4-(chloroacetylamido)butylamide
-
-
N-carbobenzyloxy-L-phenylalanine 6-(acrylamido)hexylamide
-
-
N-carbobenzyloxy-L-phenylalanine 6-(chloroacetylamido)hexylamide
-
-
N-carbobenzyloxy-L-phenylalanine 8-(acrylamido)octylamide
-
-
N-iodoacetyl-N'-(5-sulfo-1-naphthyl)ethylenediamine
-
0.01 mM, 91% and 92% inhibition of chondrosarcoma transglutaminases B and C respectively
N-[(2-phenylethoxy)carbonyl]-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(2S)-4-[(3-methoxy-1,2,4-thiadiazol-5-yl)amino]-2-[(phenoxycarbonyl)amino]butanoyl]glycine
-
irreversible, ratio kinact to Ki 0.71 micromol per min
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-5-fluoro-Na-[(quinolin-3-ylmethoxy)carbonyl]-L-tryptophanamide
-
-
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-5-fluoro-Na-[(quinolin-3-ylmethoxy)carbonyl]tryptophanamide
-
-
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[(2-phenylethoxy)carbonyl]-L-tyrosinamide
-
irreversible
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[(naphthalen-2-yloxy)carbonyl]-L-tyrosinamide
-
irreversible
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[(pyridin-3-ylmethoxy)carbonyl]-L-tyrosinamide
-
irreversible
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[(pyridin-4-ylmethoxy)carbonyl]-L-tyrosinamide
-
irreversible
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[[(1,1-dioxido-1-benzothiophen-2-yl)methoxy]carbonyl]-5-hydroxy-L-tryptophanamide
-
irreversible
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[[(1,1-dioxido-1-benzothiophen-2-yl)methoxy]carbonyl]-L-tyrosinamide
-
irreversible
N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-Nalpha-[[5-(dimethylamino)naphthalen-2-yl]sulfonyl]-L-tyrosinamide
-
study on pharmacokinetics, pharmacodynamics, and bioavailability
N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-5-[[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(pyridin-2-yl)acetamido]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-2-yl)acetamido]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-3-yl)acetamido]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
N-[(6Z)-8-amino-2-[[(benzyloxy)carbonyl]amino]-8-oxooct-6-enoyl]glycine
-
-
N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(benzyloxy)carbonyl]-3-[(prop-2-enoyl)amino]-L-alanine
-
-
N-[(benzyloxy)carbonyl]-L-alanyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(benzyloxy)carbonyl]-L-alpha-aspartyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(benzyloxy)carbonyl]-L-isoleucyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-5-oxo-6-[(1,3,4,5-tetramethyl-1H-imidazol-3-ium-2-yl)sulfanyl]-L-norleucine
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-6-(diethylsulfonio)-5-oxo-L-norleucine
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[(benzyloxy)carbonyl]glycyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N-[4-(4-cyclopentanecarbonylpiperazine-1-sulfonyl)-phenyl]acrylamide
-
N-[4-(4-cyclopropanecarbonylpiperazine-1-sulfonyl)-phenyl]acrylamide
-
N-[4-(4-phenylpiperazine-1-sulfonyl)phenyl]acrylamide
-
N-[4-(4-pyridin-2-ylpiperazine-1-sulfonyl)phenyl]acrylamide
-
N-[4-(aminomethyl)benzyl]-3-(5-[[[[(E)-2-phenylethenyl]sulfonyl](pyridin-2-ylmethyl)amino]methyl]-1,2,4-oxadiazol-3-yl)benzamide
-
N-[4-(piperazine-1-sulfonyl)phenyl]acrylamide
-
N-[4-(pyrrolidine-1-sulfonyl)phenyl]acrylamide
-
N-[4-methanesulfonylphenyl]acrylamide
-
N-[4-methoxyphenyl]acrylamide
-
N-[4-nitrophenyl]acrylamide
-
N-[4-phenoxyphenyl]acrylamide
-
N-[4-trifluoromethylphenyl]acrylamide
-
N-[4-[(1E)-3-oxo-3-(pyridin-3-yl)prop-1-en-1-yl]phenyl]acetamide
-
reversible, competitive with the acyl donor substrate
N-[4-[4-(2-phenylcyclopropanecarbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
-
N-[4-[4-(2-trifluoromethylphenyl)piperazine-1-sulfonyl]-phenyl]acrylamide
-
N-[4-[4-(3-methylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]-acrylamide
-
N-[4-[4-(3-phenylpropionyl)piperazine-1-sulfonyl]phenyl]-acrylamide
-
N-[4-[4-(3-phenylpropyl)piperazine-1-sulfonyl]phenyl]-acrylamide
-
N-[4-[4-(3-trifluoromethylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]acrylamide
-
N-[4-[4-(4,4-difluoropiperidine-1-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
-
N-[4-[4-(4-phenylbutyl)piperazine-1-sulfonyl]phenyl]-acrylamide
-
N-[4-[4-(6-methylpyridin-2-yl)piperazine-1-sulfonyl]phenyl]-acrylamide
-
N-[4-[4-(6-trifluoromethylpyridin-3-yl)piperazine-1-sulfonyl]phenyl]acrylamide
-
N-[4-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide
-
N-[4-[4-(octahydroisoquinoline-2-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
-
N-[4-[4-(octahydroquinoline-1-carbonyl)piperazine-1-sulfonyl]phenyl]acrylamide
-
N-[4-[4-(piperidine-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide
-
N-[4-[4-(pyrrolidine-1-carbonyl)piperazine-1-sulfonyl]-phenyl]acrylamide
-
N-[5-(4-cyclopropanecarbonylpiperazine-1-sulfonyl)-pyridin-2-yl]acrylamide
-
N-[5-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-pyridin-2-yl]acrylamide
-
N-[5-[4-(adamantane-1-carbonyl)piperazine-1-sulfonyl]-pyrimidin-2-yl]acrylamide
-
N-[[(5S)-3-bromo-4,5-dihydroisoxazol-5-yl]methyl]-5-fluoro-Na-[(quinolin-3-ylmethoxy)carbonyl]-L-tryptophanamide
-
-
N-{[(5S)-3-bromo-4,5-dihydro-1,2-oxazol-5-yl]methyl}-5-fluoro-Nalpha-[(quinolin-3-ylmethoxy)carbonyl]-L-tryptophanamide
-
N2-[(benzyloxy)carbonyl]-L-lysyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
N2-[(benzyloxy)carbonyl]-N5-prop-2-enoyl-L-ornithine
-
-
N2-[(benzyloxy)carbonyl]-N6-(prop-2-enoyl)-L-lysylglycine
-
-
N2-[(benzyloxy)carbonyl]-N6-prop-2-enoyl-L-lysinamide
-
-
N2-[(benzyloxy)carbonyl]-N6-prop-2-enoyl-L-lysine
-
-
N5-(3-methoxy-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-ornithylglycine
-
irreversible, ratio kinact to Ki 0.55 micromol per min
N6-(3-methoxy-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-lysylglycine
-
irreversible, ratio kinact to Ki 0.72 micromol per min
Na+
-
1 mM, 57% inhibition
Na-[(benzyloxy)carbonyl]-N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-5-fluorotryptophanamide
-
-
Nalpha-[(benzyloxy)carbonyl]-N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-L-tyrosinamide
naphthoquinone
-
0.015 mM, complete inhibition
NC-I052
irreversible inhibitor
NC9
potent inhibitor, NC9 inhibiting osteoclastogenesis, also inhibits differentiation, migration, and fusion of pre-osteoclasts as well as resorption activity of mature osteoclasts. NC9 increases RhoA levels and blocks podosome belt formation. The number of TRAP+ mononuclear pre-osteoclasts is significantly decreased by NC9 treatment for the first 2 days. The inhibitory effect ofNC9 on osteoclastogenesis as well as podosome belt formation is completely reversed with a Rho-family inhibitor Exoenzyme C3. Microtubule architecture, acetylation, and detyrosination of alpha-tubulin are not affected; potent inhibitor, NC9 inhibiting osteoclastogenesis, also inhibits differentiation, migration, and fusion of pre-osteoclasts as well as resorption activity of mature osteoclasts. NC9 increases RhoA levels and blocks podosome belt formation. The number of TRAP+ mononuclear pre-osteoclasts is significantly decreased by NC9 treatment for the first 2 days. The inhibitory effect ofNC9 on osteoclastogenesis as well as podosome belt formation is completely reversed with a Rho-family inhibitor Exoenzyme C3. Microtubule architecture, acetylation, and detyrosination of alpha-tubulin are not affected; potent inhibitor, NC9 inhibiting osteoclastogenesis, also inhibits differentiation, migration, and fusion of pre-osteoclasts as well as resorption activity of mature osteoclasts. NC9 increases RhoA levels and blocks podosome belt formation. The number of TRAP+ mononuclear pre-osteoclasts is significantly decreased by NC9 treatment for the first 2 days. The inhibitory effect ofNC9 on osteoclastogenesis as well as podosome belt formation is completely reversed with a Rho-family inhibitor Exoenzyme C3. Microtubule architecture, acetylation, and detyrosination of alpha-tubulin are not affected
NEM
-
34.38% activity remaining at 10 mM
o-phenanthroline
-
not reversible by Ca2+
ornithine
-
weak, suicide substrate in the presence of casein
Pb(CH3COO)2
-
1 mM, 56% inhibition
Pb2+
-
5 mM Pb(CH3COO)2, 80% inhibition
PCMB
-
1.62% activity remaining at 10 mM
phenyl methyl sulfonyl fluoride
-
10 mM, complete inhibition
PMSF
-
40.79% activity remaining at 10 mM
pyrrolidine-1-carboxylic acid (4-acryloylaminophenyl)-amide
-
quinolin-3-ylmethyl [(1S)-2-([[(5S)-3-bromo-4,5-dihydroisoxazol-5-yl]methyl]amino)-1-(4-hydroxybenzyl)-2-oxoethyl]carbamate
-
-
quinolin-3-ylmethyl [(1S)-2-[[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]amino]-1-(4-hydroxybenzyl)-2-oxoethyl]carbamate
-
-
R281
irreversible inhibitor
-
S-nitroso-N-acetylpenicillamine
-
NO-donor, 8-16 mM, almost complete inhibition of transglutaminases 1 and 3, weak inhibition of transglutaminase 3
Sodium citrate
-
above 10 mM, complete inactivation
SQAETYR
-
noncompetitive inhibition
SYAETYR
-
noncompetitive inhibition
Tb3+
-
noncompetitive inhibition of factor XIIIa, at high Ca2+-levels, not reversed by Ca2+
tert-butyl 3-(3-fluorophenyl)-2-[(2-hydrazino-2-oxoethyl)sulfanyl]-4-oxo-3,5,6,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine-7(4H)-carboxylate
-
-
tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
tert-butyl N-(3-methyl-1,2,4-thiadiazol-5-yl)-N2-(phenoxycarbonyl)-L-glutaminylglycinate
-
irreversible, ratio kinact to Ki 0.78 micromol per min
tert-butyl N6-acryloyl-N2-[(benzyloxy)carbonyl]-L-lysylglycinate
-
tert-butyl [4-[(1E)-3-(1H-benzotriazol-1-yl)-3-oxoprop-1-en-1-yl]phenyl]carbamate
-
reversible, competitive with the acyl donor substrate
tetrathionate
-
inactivation, not reversible by dithiothreitol
tricyclo[3.3.1.13,7]dec-1-ylmethyl bromoacetate
-
-
tricyclo[3.3.1.13,7]dec-1-ylmethyl prop-2-enoate
-
-
UTP
-
50% as effective as ATP
VA4
-
the inhibitor also inhibits epidermal cancer stem cell invasion with an EC50 of 0.0039 mM
vitamin K1
-
0.015 mM, 10% inhibition
vitamin K2
-
0.015 mM, 75% inhibition
Z-DON-Val-Pro-Leu-OMe
-
irreversible inhibitor
ZED1227
an irreversible peptidomimetic TG2-selective inhibitor
[(2-[[(benzyloxy)carbonyl]amino]-4-[5-(formylamino)-1,2,4-thiadiazol-3-yl]butanoyl)amino]acetic acid
-
-
[(4-[3-(aminocarbonyl)oxiran-2-yl]-2-[[(benzyloxy)carbonyl]amino]butanoyl)amino]acetic acid
-
-
[(5R,8S)-8-{[(benzyloxy)carbonyl]amino}-5-(methoxycarbonyl)-2,7-dioxo-9-phenylnonyl](dimethyl)sulfonium bromide
-
[([3-(aminocarbonyl)oxiran-2-yl][[(benzyloxy)carbonyl]amino]acetyl)amino]acetic acid
-
-
[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-ylmethyl]-carbamic acid benzyl ester
-
[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-yl]-carbamic acid benzyl ester
-
[2-[(2-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-2-oxoethyl)amino]-2-oxoethyl](dimethyl)sulfanium
-
-
[2-[(3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-2,3-dioxopropyl)amino]-2-oxoethyl](diethyl)sulfanium bromide
-
-
[2-[(3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-2,3-dioxopropyl)amino]-2-oxoethyl](dimethyl)sulfanium bromide
-
-
[2-[(4-acryloylaminobenzenesulfonyl)methylamino]ethyl]-methylcarbamic acid benzyl ester
-
[4-(4-acryloylpiperazine-1-sulfonyl)phenyl]carbamic acid benzyl ester
-
[4-[(4-aminophenyl)sulfonyl]piperazin-1-yl](cyclopropyl)methanone
-
[[(4E)-6-amino-2-[[(benzyloxy)carbonyl]amino]-6-oxohex-4-enoyl]amino]acetic acid
-
-
[[(5E)-7-amino-2-[[(benzyloxy)carbonyl]amino]-7-oxohept-5-enoyl]amino]acetic acid
-
-
[[(6Z)-8-amino-2-[[(benzyloxy)carbonyl]amino]-8-oxooct-6-enoyl]amino]acetic acid
-
-
(NH4)2SO4
-
65.58% activity remaining at 10 mM
(NH4)2SO4
Nemipterus sp.
-
-
1-(6-methylpyridin-2-yl)piperazine
-
1-(6-methylpyridin-2-yl)piperazine
-
1-(6-nitropyridin-3-yl)piperazine
-
1-(6-nitropyridin-3-yl)piperazine
-
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
-
2-([3-(2-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
50% inhibition at 0.00025 mM, standard format, at 0.00018 mM, full progress curve
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
-
2-([3-(3-fluorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
50% inhibition at 0.00021 mM, standard format, at 0.00014 mM, full progress curve
3-iodo-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
3-iodo-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
3-[benzyl(tert-butyl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
-
-
3-[benzyl(tert-butyl)amino]-1-(5-bromothiophen-2-yl)propan-1-one
-
4-fluoro-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
4-fluoro-N-[(2S)-1-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
4-fluoro-N-[(2S)-1-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
4-fluoro-N-[(2S)-1-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-1-oxo-6-[(prop-2-enoyl)amino]hexan-2-yl]benzamide
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
1 mol per mol enzyme, 85% inactivation, not reversed by glutathione
5,5'-dithiobis(2-nitrobenzoic acid)
-
irreversible, carbobenzoxy-Phe protects
5,5'-dithiobis(2-nitrobenzoic acid)
-
reversed by dithiothreitol
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
-
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxamide
-
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
-
5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylic acid
-
ADP
-
complete inhibition of rat liver and human brain transglutaminase, reversible, non-competitive to putrescine
ADP
-
complete inhibition of rat liver and human brain transglutaminase, reversible, non-competitive to putrescine
ATP
-
3 mM, complete inhibition of rat liver and human brain tissue-type transglutaminase, reversible; 3 mM, complete inhibition of rat liver and human brain transglutaminase, reversible, non-competitive to putrescine
ATP
-
0.5 mM, approx. 60% inhibition of recombinant tranglutaminase
ATP
-
3 mM, complete inhibition of rat liver and human brain tissue-type transglutaminase, reversible; 3 mM, complete inhibition of rat liver and human brain transglutaminase, reversible, non-competitive to putrescine
ATP
-
2 mM, 27% inhibition
Ba2+
-
22.55% activity remaining at 10 mM
Ba2+
-
10 mM, complete inhibition
cadaverine
-
complete inhibition at 0.15 mM
cadaverine
-
strong, putrescine as substrate
cadaverine
-
2 mM, 70% inhibition
chlorpromazine
-
reverses calmodulin enzyme stimulation
chlorpromazine
-
reverses calmodulin enzyme stimulation
CTP
-
3 mM, complete inhibition of rat liver and human brain transglutaminase, reversible, non-competitive to putrescine
CTP
-
3 mM, complete inhibition of rat liver and human brain transglutaminase, reversible, non-competitive to putrescine
Cu2+
-
-
Cu2+
-
KCN or dithiothreitol restore activity; mechanism
Cu2+
-
19.78% activity remaining at 10 mM
Cu2+
-
strong inactivation
Cu2+
-
10 mM, complete inhibition
Cu2+
-
trace amounts, 0.45 mM diethyldithiocarbamate stimulates crude preparation
Cu2+
-
5 mM CuSO4, 91% inhibition
Cu2+
-
1 mM, complete inhibition
cystamine
-
50% inhibition at 0.022 mM
cystamine
-
transglutaminase inhibitor cystamine alleviates the abnormality in liver from NZB/W F1 mice
cystamine
-
significant reduction in TG2 activity in NZB/W F1 mice following cystamine administration
cystamine
-
2 mM, 58% inhibition
cystamine
-
ameliorates liver fibrosis induced by carbon tetrachloride via inhibition of tissue transglutaminase
Dansylcadaverine
-
0.0019 mM, 50% inhibition
Dansylcadaverine
-
0.0019 mM, 50% inhibition
EDTA
-
-
EDTA
complete inhibition at 10 mM
EDTA
complete inhibition at 10 mM
EDTA
the enzyme is inhibited at 10 mM
EDTA
-
10 mM, complete inhibition
EDTA
complete inhibition at 10 mM
EDTA
-
1 mM, stable in absence of NaCl, inactivation in presence of NaCl
EDTA
-
10 mM, no residual activity
EDTA
-
complete inactivation above 10 mM
EDTA
-
5 mM; 5 mM, complete inhibition
EGTA
-
2.5 mM, 94% inhibition
EGTA
-
42.93% activity remaining at 10 mM
EGTA
-
10 mM, complete inhibition
EGTA
-
2 mM, irreversible
EGTA
-
weak, reversible by Ca2+
EGTA
-
5 mM, 100% inhibition
ERW1041E
-
i.e. (S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
Fe2+
-
-
GDP
-
inhibits hydrolysis of GTP
GDP
-
inhibits hydrolysis of GTP
GDP
-
at low levels of Ca2+
GTP
-
weak inhibition in the millimolar range
GTP
-
inhibition of tissue transglutaminase
GTP
-
inhibition of tissue transglutaminase
GTP
-
0.1 mM, complete inhibition at suboptimal Ca2+-levels
GTP
-
50% as effective as ATP
GTP
-
0.02-0.1 mM, inhibition of transglutaminases 2 and 3
GTP
-
causes significant shifts in electrophoretic mobility of the protein under native conditions
GTP
the protein transamidase activity of TG2 is positively regulated by calcium and negatively regulated by GTP
GTP
-
inhibition of tissue transglutaminase
GTP
-
0.005 mM, complete inhibition
GTP
-
0.05 mM, 50% inhibition of lens transglutaminase, 0.5 mM, complete inhibition in the presence of 0.5 mM Ca2+, increasing the Ca2+ concentration to 3 mM reverses inhibition
GTP
-
0.5 mM, almost complete inhibition of recombinant transglutaminase in the presence of 0.5 mM Ca2+, no inhibition in the presence of 2 mM Ca2+
GTP
-
inhibition of tissue transglutaminase
GTP
-
50% as effective as ATP
GTP
-
2 mM, 80% inhibition
GTP-gamma-S
-
inhibition of GTP-hydrolysis
GTP-gamma-S
-
inhibition of GTP-hydrolysis
GTP-gamma-S
1 mM, 60% inhibition of transglutaminase activity in presence of 0.5 mM Ca2+, 0.1 mM, 50% inhibition of GTPase activity
Hg2+
-
-
Hg2+
-
5 mM HgCl2, 94% inhibition
iodoacetamide
-
complete inhibition at 50 mM
iodoacetamide
-
10 mM, 62% inhibition in the presence of 10 mM Ca2+
iodoacetamide
-
0.1 mM, pH 6.8, in the presence of Ca2+, complete inhibition, irreversible, incorporation of 1 mol carbamidomethyl/mol enzyme, substrate protects
iodoacetamide
-
0.1 mM, pH 6.8, in the presence of Ca2+, complete inhibition, irreversible, incorporation of 1 mol carbamidomethyl/mol enzyme, substrate protects; mechanism
iodoacetamide
irreversible inhibition
iodoacetamide
-
factor XIIIa; not inhibited in the absence of Ca2+, calmodulin regulated transglutaminases is not inhibited
iodoacetamide
-
factor XIIIa; not inhibited in the absence of Ca2+, calmodulin regulated transglutaminases is not inhibited
iodoacetamide
-
0.1 mM and 1 mM for normal skin and keloid scar, respectively
iodoacetamide
-
1 mM, 89% inhibition of DEAE-absorbed transglutaminase
iodoacetamide
-
86% and 91% inhibition of chondrosarcoma transglutaminase B and C respectively
iodoacetic acid
-
28.75% activity remaining at 10 mM
iodoacetic acid
-
10 mM, complete inhibition
KCC009
-
inhibition of enzyme and subsequent block of fibronectin assembly in the extracellular matrix of glioblastoma cells
KCC009
-
dihydroisoxazole TG2 inhibitor
KCC009
a specific tTG inhibitor
KCC009
-
inhibition of enzyme and subsequent block of fibronectin assembly in the extracellular matrix of glioblastoma cells in vitro and in vivo. KCC009 treatment in mice harboring orthotopic glioblastomas sensitizes the tumors to N,N-bis(2-chloroethyl)-N-nitrosourea chemotherapy
KCl
-
45% activity at 400 mM
LDN-27219
-
reversible, slow-binding inhibitor that appears not to bind at the enzymes active site but rather at the enzymes GTP site, or a site that regulates binding of GTP. The potency and kinetics of inhibition are dependent on substrate structure and suggest a novel mechanism of inhibition that involves differential binding of LDN-27219 to multiple conformational states of this enzyme
methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
-
methyl 5-[4-[N2-(phenylacetyl)-N6-(prop-2-enoyl)-L-lysyl]piperazin-1-yl]pyridine-2-carboxylate
-
methylamine
-
1.8 mM, 50% inhibition
methylamine
-
1.8 mM, 50% inhibition
Mg2+
-
53.52% activity remaining at 10 mM
Mg2+
-
significant inhibition
Mg2+
-
1 mM, complete inhibition
Mn2+
-
30.65% activity remaining at 10 mM
monodansyl cadaverine
MDC
monodansyl cadaverine
-
-
Monodansylcadaverine
-
-
Monodansylcadaverine
treatment of proximal renal tublule cells with inhibitor monodansylcadaverine or siRNA results in decreased proliferation accompanied by activation of signal transducer and activator of transcription, Akt and Stat-3. Treatment with monodansylcadaverine or TGase-1 siRNA decreases Stat-3 but not Akt phosphorylation. TGase-1 interacts with Janus-activated kinase JAK2, and this interaction is inhibited by monodansylcadaverine
Monodansylcadaverine
-
partial inhibition above 0.5 mM
Monodansylcadaverine
-
2 mM, 97% inhibition
Monodansylcadaverine
-
inhibition of glutamyl transfer to putrescine-pectin and putrescine-alginate
monoiodoacetate
-
1 mM, 97% inhibition
monoiodoacetate
-
1 mM, 93% inhibition of DEAE-unabsorbed transglutaminase, 85% inhibition of DEAE-absorbed transglutaminase
monoiodoacetate
-
1 mM, 24% inhibition
monoiodoacetate
-
1 mM, 94% inhibition
N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
-
N,N-dimethyl-5-(piperazine-1-sulfonyl)naphthalen-1-amine
-
N-ethylmaleimide
-
3.6 mol per mol enzyme, 91% inhibition in the presence of Ca2+, not inhibited in the absence of Ca2+, substrate protects
N-ethylmaleimide
-
1 mM, 75% inhibition
N-ethylmaleimide
-
0.1 mM, 60% inhibition
N-ethylmaleimide
-
strong inactivation in the presence of Ca2+, not inhibited in the absence of Ca2+
N-ethylmaleimide
-
strong inactivation
N-ethylmaleimide
Nemipterus sp.
-
-
N-ethylmaleimide
-
10 mM, complete inhibition
N-ethylmaleimide
-
1 mM, complete inhibition of DEAE-unabsorbed transglutaminase, 93% inhibition of DEAE-absorbed transglutaminase
N-ethylmaleimide
-
0.1 mM
N-ethylmaleimide
-
irreversible inhibition, inhibition increases with increasing Ca2+ concentrations, 50% inhibition at 1 mM Ca2+
N-ethylmaleimide
-
79% inactivation
N-ethylmaleimide
-
5 mM, strong
N-ethylmaleimide
strong inhibition
N-ethylmaleimide
-
1 mM, 90% inhibition
N-ethylmaleimide
-
1 mM, 98% inhibition
N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-(2-cyclohexylacetamido)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(2-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(3-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-bromophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-chlorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-fluorophenyl)acetamido]-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-iodophenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[2-(4-methylphenyl)acetamido]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[(4-fluorophenyl)carbamothioyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[(4-fluorophenyl)carbamoyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[(4-fluorophenyl)methyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-5-[[5-(dimethylamino)naphthalene-1-sulfonyl]amino]-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxohexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-(4-phenylpiperazin-1-yl)hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-2-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-3-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-(pyridin-4-yl)piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-5-(2-phenylacetamido)-6-[4-[6-(trifluoromethyl)pyridin-3-yl]piperazin-1-yl]hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-oxo-6-[4-(6-phenylpyridin-2-yl)piperazin-1-yl]-5-(2,2,2-trifluoroacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(3-methylphenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(4-fluorobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(4-nitrobenzoyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(4-nitrophenyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-bromopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-chloropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-chloropyridine-2-carbonyl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
determination of the thermodynamic solubility of the compound
N-[(5S)-6-[4-(6-fluoropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
determination of the thermodynamic solubility of the compound
N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-fluoropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-iodopyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
an selective Nepsilon-acryloyllysine derivative, irreversible inhibition
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
reversible inhibitor
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
reversible inhibitor
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamothioyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[(phenylmethanesulfonyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(pyridin-2-yl)acetamido]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(pyridin-2-yl)acetamido]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-2-yl)acetamido]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-2-yl)acetamido]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-3-yl)acetamido]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-[2-(thiophen-3-yl)acetamido]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
determination of the thermodynamic solubility of the compound
N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
determination of the thermodynamic solubility of the compound
N-[(5S)-6-[4-(6-nitropyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
reversible inhibitor
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
reversible inhibitor
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-nitropyridin-3-yl)piperazin-1-yl]-6-oxo-5-[(phenylcarbamoyl)amino]hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-(6-tert-butylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-[(4-fluorophenyl)methyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
N-[(5S)-6-[4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
NaCl
-
20% inhibition at 15 mM
NaCl
-
500 mM, 2 h at 20°C in the absence of substrate, 86% inhibition, reversible to some extent by dilution
NaCl
Nemipterus sp.
-
1.2 M, 25% inhibition
NaCl
-
500 mM, 58% inhibition
Nalpha-[(benzyloxy)carbonyl]-N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-L-tyrosinamide
-
-
Nalpha-[(benzyloxy)carbonyl]-N-[(3-bromo-4,5-dihydroisoxazol-5-yl)methyl]-L-tyrosinamide
-
study on pharmacokinetics, pharmacodynamics, and bioavailability
NH4+
-
5 mM, 36% inhibition
NH4+
-
complete inhibition of coagulating gland transglutaminase with more than 1 mM NH4Cl or 20 mM (NH4)2SO4
p-chloromercuribenzoate
-
reversible by glutathione
p-chloromercuribenzoate
-
-
p-chloromercuribenzoate
-
1 mM, 98% inhibition
p-chloromercuribenzoate
-
strong inactivation
p-chloromercuribenzoate
-
10 mM, complete inhibition
p-chloromercuribenzoate
-
0.1 mM
p-chloromercuribenzoate
-
21% inhibition of chondrosarcoma transglutaminase B
p-chloromercuribenzoate
-
1 mM, 44% inhibition
putrescine
-
-
putrescine
-
pan-transglutaminase inhibition inhibits terminal differentiation of keratinocytes, leading to a hyperproliferative epidermis with parakeratosis and enhanced expression of involucrin and cytokeratins 6 and 16. Expression of the differentiation-associated cytokeratin, cytokeratin 10, is reduced. Basement membrane integrity is also lost as a result of transglutaminase inhibition
putrescine
-
0.1-0.2 mM, substrate inhibition
putrescine
-
2 mM, 75% inhibition
R283
irreversible inhibitor
R283
-
specific inhibitor, i.e. 1,3-dimethyl-2-[(2-oxopropyl)thio]imidazolium chloride, complete inhibition at 0.25 mM
spermidine
-
-
spermidine
-
0.1-0.2 mM, substrate inhibition
spermidine
-
2 mM, 70% inhibition
spermine
-
0.17 mM, 50% inhibition
spermine
-
0.1-0.2 mM, substrate inhibition
spermine
-
0.17 mM, 50% inhibition
spermine
-
2 mM, 68% inhibition
tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
-
tert-butyl 4-(4-fluorobenzoyl)piperazine-1-carboxylate
-
tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
-
tert-butyl 4-(4-nitrobenzoyl)piperazine-1-carboxylate
-
tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
-
tert-butyl 4-(6-chloropyridine-2-carbonyl)piperazine-1-carboxylate
-
tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-fluoropyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-fluoropyridin-3-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-iodopyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-nitropyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-phenylpyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(6-tert-butylpyridin-2-yl)piperazine-1-carboxylate
-
tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
-
tert-butyl 4-(pyridin-3-yl)piperazine-1-carboxylate
-
tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
-
tert-butyl 4-[(4-fluorophenyl)methyl]piperazine-1-carboxylate
-
tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
-
tert-butyl 4-[6-(2-fluoroethoxy)pyridin-2-yl]piperazine-1-carboxylate
-
tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
-
tert-butyl 4-[6-(methoxycarbonyl)pyridin-3-yl]piperazine-1-carboxylate
-
tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
-
tert-butyl 4-[6-(trifluoromethyl)pyridin-3-yl]piperazine-1-carboxylate
-
Zn2+
-
-
Zn2+
-
20.12% activity remaining at 10 mM
Zn2+
-
10 mM, complete inhibition
Zn2+
-
5 mM ZnSO4, 95% inhibition
Zn2+
-
1 mM, 89% inhibition
ZnCl2
-
5 mM, 97.5% inhibition, 43% inhibition in the presence of 10 mM Ca2+
additional information
-
not inhibited by mono- and dimethylated dansylcadaverine
-
additional information
-
-
-
additional information
-
-
-
additional information
-
rapid degradation of liver tissue transglutaminase in the presence of micro-calpain, GTP-gamma-S inhibits degradation
-
additional information
-
not inhibitory: beta-mercaptoethanol
-
additional information
-
not inhibitory: N-carbobenzyloxy-L-phenylalanine 2-(chloroacetylamido)ethylamide
-
additional information
-
beta-aminoethyl ketones strongly inhibit TGase, alpha- and gamma-aminoalkyl ketones show very weak TGase inhibition
-
additional information
Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
additional information
-
rapid inactivatin of factor XIIIa by trypsin and thrombin in the absence of metal ions
-
additional information
-
-
-
additional information
-
-
-
additional information
-
-
-
additional information
-
transglutaminase 1, not inhibited by GTP
-
additional information
-
inhibitory activity in decreasing order: cystamine, spermidine, spermine, putrescine, cysteamine
-
additional information
peptide harboring Gln mimics, e.g. 6-diazo-5-oxo-L-norleucine, have the potential to show considerably higher specificity for TG2 than the amine inhibitors. Non-hydrolyzable GTP analogs (e.g. 5'-guanylyl imidodiphosphate) are also inhibitors of TG2 activity. Because of the tight coupling between the GTP binding site and the transamidase/deamidase active site of TG2, these ligands act as competitive inhibitors of both the GTPase and transglutaminase activities of this enzyme
-
additional information
-
peptide harboring Gln mimics, e.g. 6-diazo-5-oxo-L-norleucine, have the potential to show considerably higher specificity for TG2 than the amine inhibitors. Non-hydrolyzable GTP analogs (e.g. 5'-guanylyl imidodiphosphate) are also inhibitors of TG2 activity. Because of the tight coupling between the GTP binding site and the transamidase/deamidase active site of TG2, these ligands act as competitive inhibitors of both the GTPase and transglutaminase activities of this enzyme
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
-
poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor; poor inhibition by ZED1227, an irreversible peptidomimetic TG2-selective inhibitor
-
additional information
-
efficient site-specific antibody-drug conjugation by engineering a nature-derived recognition tag for microbial transglutaminase, overview. Synthesis and evaluation of series of targeted covalent inhibitors (TCIs) whose structure is based on a Cbz-Lys scaffold, the irreversible inhibitors block both the transamidation and GTP-binding activities of hTG2, structure-activity relationship (SAR) study and docking study using crystal structure PDB ID 2Q3Z. Isozyme selectivity. No inhibition by benzyl [(2S)-1-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-1-oxo-3-[(prop-2-enoyl)amino]propan-2-yl]carbamate and benzyl [(2S)-1-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-1-oxo-4-[(prop-2-enoyl)amino]butan-2-yl]carbamate
-
additional information
Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
additional information
Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
additional information
Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
additional information
Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
additional information
Nepsilon-acryloyllysine piperazides as irreversible inhibitors of transglutaminase 2, synthesis, structure-activity relationships, and pharmacokinetic profiling, overview. No inhibition by N-[(5R)-6-[4-(6-methylpyridin-2-yl)piperazin-1-yl]-6-oxo-5-(2-phenylacetamido)hexyl]prop-2-enamide
-
additional information
-
not inhibitory: didansylcadaverine
-
additional information
-
not inhibited by GDP
-
additional information
-
not inhibited by adenosine or adenine
-
additional information
-
not inhibited by mono- and dimethylated dansylcadaverine
-
additional information
-
not inhibited by diisopropylfluorophosphate; not inhibited by PMSF; not inhibited by sulfhydryl-reagents in the absence of Ca2+
-
additional information
-
transglutaminase of coagulating gland, not inhibited by GTP
-
additional information
-
the enzyme is not inhibited by ethylenediaminetetraacetic acid, Na+, K+, Ca2+, Mg2+, Ba2+, Mn2+ and Co2+
-
additional information
the amount of ammonia produced by cross-linking casein with the mutant MTG in the presence of 20% ethanol is less than the control
-
additional information
-
not inhibitory: Ba2+, Ca2+, Co2+, Cu2+, Fe2+, Fe3+, Mg2+, Mn2+, Na+, phenylmethylsulfonyl fluoride, EDTA
-
additional information
-
enzyme precursor protein is inhibitory to mature enzyme, even after heat treatment. Precursor is secreted to culture medium; heat-treated pro-enzyme acts effectively as inhibitor of mature form
-
additional information
isozyme MTG-TX is not inhibited by Li+, Na+, K+, Ca2+, Mg2+, Ba2+, Mn2+, or the inhibitor phenylmethanesulfonyl fluoride (PMSF)
-
additional information
-
not inhibited by Ba2+, Co2+, Fe3+, K+, Mg2+, Mn2+, Na+, Ni2+, Sr2+
-
additional information
-
not inhibited by diisopropylfluorophosphate
-