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2.3.2.13: protein-glutamine gamma-glutamyltransferase

This is an abbreviated version!
For detailed information about protein-glutamine gamma-glutamyltransferase, go to the full flat file.

Word Map on EC 2.3.2.13

Reaction

protein glutamine
+
alkylamine
=
protein N5-alkylglutamine
 +
NH3

Synonyms

AcTG-1, BmTGA, chloroplast transglutaminase, chlTGase, cold active transglutaminase, cold-active transglutaminase, EPB42, factor XIII, factor XIIIa, fibrin stabilizing factor, fibrinoligase, Galphah, glutamine:amine gamma-glutamyl-transferase, glutaminylpeptide gamma-glutamyltransferase, glutamyltransferase, glutaminylpeptide gamma-, gpTGase 2, gTG2, hfXIIIa, hTG2, hTGase 1, hTGase 2, hTGase 3, hTGase 6, KALB, KalbTG, KALB_7456, Laki-Lorand factor, mammalian transglutaminase, microbial transglutaminase, microbial transglutaminases, MsTGase, MTG, MTG-TX, MTGase, mTGase 2, OlTGT, plastidial transglutaminase, polyamine transglutaminase, protein 4.2, protein-glutamine gamma-glutamyltransferase, R-glutaminyl-peptide:amine gamma-glutamyl transferase, R-glutaminylpeptide-amine gamma-glutamyltransferase, SCTG, SMTG, STG I, t-TG, TG-2, TG1, TG2, TG3, TG4, TG5, TG6, TG7, tGA, TGase, TGase 1, TGase 2, Tgase 3, TGase 6, Tgase II, TGase-2, TGase2, TGB, TGK1, TGK2, TGL, TGM1, TGM2, TGM3, TGM4, TGM5, TGM6, TGM7, TGZ, tgz15, TGZo, tissue transglutaminase, tissue transglutaminase 2, tissue-TG, transglutaminase, transglutaminase 1, transglutaminase 2, transglutaminase 3, transglutaminase 6, transglutaminase C, transglutaminase factor XIII, transglutaminase type II, transglutaminase-2, transglutaminase-like protein, transglutaminase2, tTG, tTG-2, type 2 transglutaminase, type I transglutaminase, type-2 transglutaminase

ECTree

     2 Transferases
         2.3 Acyltransferases
             2.3.2 Aminoacyltransferases
                2.3.2.13 protein-glutamine gamma-glutamyltransferase

Inhibitors

Inhibitors on EC 2.3.2.13 - protein-glutamine gamma-glutamyltransferase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(1Z)-2-{[3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]sulfanyl}ethanehydrazonic acid
-
-
(2-tert-butoxy-2-oxoethyl)(dimethyl)sulfonium
-
-
(2-[[(1R)-3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-1-carboxy-3-oxopropyl]amino]-2-oxoethyl)(dimethyl)sulfanium bromide
-
-
(2-[[4-(methoxycarbonyl)benzyl]oxy]-2-oxoethyl)(dimethyl)sulfonium
-
-
(2-[[6-(methoxycarbonyl)naphthalen-2-yl]methoxy]-2-oxoethyl)(dimethyl)sulfonium
-
-
(2E)-3-(4-nitrophenyl)-1-(pyridin-3-yl)prop-2-en-1-one
-
reversible, competitive with the acyl donor substrate
(2S)-2-[[(benzyloxy)carbonyl]amino]-4-[(prop-2-enoyl)amino]butanoic acid
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(2-hydroxybenzamido)pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(3-hydroxybenzamido)pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(4-hydroxybenzamido)pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(nicotinamido)pyrrolidine-1-carboxylate
-
-
(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
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(pyrazine-2-carboxamido)-pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-fluoropyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-hydroxypyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-methoxypyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-phenylpyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 4-(benzyloxy)-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 4-amino-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 4-benzamido-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(2S,4R)-quinolin-3-ylmethyl 4-benzyl-2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(2-hydroxyphenyl)pyrrolidine-1-carboxylate
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(3-chlorophenyl)pyrrolidine-1-carboxylate
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(3-hydroxyphenyl)pyrrolidine-1-carboxylate
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(4-chlorophenyl)pyrrolidine-1-carboxylate
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-(4-hydroxyphenyl)pyrrolidine-1-carboxylate
-
-
(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
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-fluoropyrrolidine-1-carboxylate
-
-
(2S,4S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-4-phenylpyrrolidine-1-carboxylate
-
-
(3E)-1-benzyl-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-3-(2-oxopropylidene)-6-(trifluoromethoxy)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-3-[2-(3-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
-
-
(3E)-3-[2-(4-aminophenyl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
-
-
(3E)-3-[2-(5-bromopyridin-3-yl)-2-oxoethylidene]-4-chloro-1,3-dihydro-2H-indol-2-one
-
-
(3E)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-1-(2-methylpropyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-1-(cyclohexylmethyl)-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-1-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-(2-oxo-2-phenylethylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-(2-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-(3-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-(3-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-(4-chlorophenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-(4-methoxyphenyl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-(6-methoxypyridin-3-yl)-2-oxoethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-2-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(2-phenylethyl)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(3-phenylpropyl)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-(propan-2-yl)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1-phenyl-1,3-dihydro-2H-indol-2-one
-
-
(3E)-4-chloro-3-[2-oxo-2-(pyridin-4-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-5-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-5-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-5-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-5-methyl-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-5-nitro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-6-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-6-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-6-fluoro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-7-bromo-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(3E)-7-chloro-3-(2-oxopropylidene)-1,3-dihydro-2H-indol-2-one
-
-
(3E)-7-chloro-3-[2-oxo-2-(pyridin-3-yl)ethylidene]-1,3-dihydro-2H-indol-2-one
-
-
(4R)-1-[(benzyloxy)carbonyl]-4-hydroxy-L-prolyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
(5-bromothiophen-2-yl)(4-methyl-1H-pyrazol-1-yl)methanone
-
(E)-1-(1-(2-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
(E)-1-(1-(3-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
(E)-1-(1-(4-nitrobenzyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
(E)-1-(1-(cyclohexylmethyl)-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
(E)-1-(1-benzyl-1H-1,2,3-triazol-4-yl)-3-(4-nitrophenyl)prop-2-en-1-one
-
(naphthalen-2-yl)methyl 4-(N-acryloylglycyl)piperazine-1-carboxylate
-
-
(naphthalen-2-yl)methyl 4-[N-(bromoacetyl)glycyl]piperazine-1-carboxylate
-
-
(NH4)2SO4
(R)-quinolin-3-ylmethyl 3-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(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
-
-
(S)-(1H-benzo[d]imidazol-2-yl)methyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-(R)-1-(naphthalen-2-yl)ethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-(R)-1-(quinolin-3-yl)ethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-(S)-1-(naphthalen-2-yl)ethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-2,3-dimethoxybenzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-3-(benzyloxy)benzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-3-fluorobenzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-4-ethynylbenzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-benzyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-N-(((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-2-(1-(dimethylamino)naphthalene-5-sulfonamido)-3-(1H-indol-3-yl)propanamide
-
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
-
-
(S)-prop-2-yn-1-yl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-pyridin-2-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-pyridin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-pyridin-4-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)-methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)-4-phenyl-2,5-dihydro-1H-pyrrole-1-carboxylate
-
-
(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)-2-methylpyrrolidine-1-carboxylate
-
-
(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)azetidine-1-carboxylate
-
-
(S)-quinolin-3-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)piperidine-1-carboxylate
-
-
(S)-quinolin-3-ylmethyl 2-(2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)amino)-2-oxoethyl)pyrrolidine-1-carboxylate
-
-
(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
-
-
(S)-quinolin-4-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-quinoxalin-2-ylmethyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)carbamoyl)pyrrolidine-1-carboxylate
-
-
(S)-tert-butyl 2-((((S)-3-bromo-4,5-dihydroisoxazol-5-yl)methyl)-carbamoyl)pyrrolidine-1-carboxylate
-
-
1,1'-methanediylbis(1H-indole-2,3-dione)
-
-
1,1'-[(2,5-dimethylbenzene-1,4-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
-
-
1,1'-[(4,6-dimethylbenzene-1,3-diyl)dimethanediyl]bis(1H-indole-2,3-dione)
-
-
1,3-dimethyl-2-[(2-oxopropyl)thio]-1H-imidazol-3-ium
-
-
1,3-dimethyl-2-[(2-oxopropyl)thio]imidazolium
-
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
-
-
1-(1-benzothiophen-2-yl)-3-[benzyl(tert-butyl)amino]propan-1-one
-
-
1-(6-methylpyridin-2-yl)piperazine
1-(6-nitropyridin-3-yl)piperazine
1-(ethenylsulfonyl)tricyclo[3.3.1.13,7]decane
-
-
1-(furan-2-yl)-3-[(2-hydroxyethyl)(propan-2-yl)amino]propan-1-one
-
-
1-(tricyclo[3.3.1.13,7]dec-1-yl)prop-2-en-1-one
-
-
1-acetyl-L-prolyl-6-imino-5-oxo-L-norleucyl-L-leucyl-L-prolyl-L-phenylalaninamide
-
1-ethyl-3-(4-methoxyphenyl)-6-methylpyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione
-
1-[(2E)-3-(4-nitrophenyl)prop-2-enoyl]-3H-[1,2,3]triazolo[4,5-b]pyridin-1-ium-3-olate
-
reversible, competitive with the acyl donor substrate
1-[(benzyloxy)carbonyl]-L-prolyl-6-(dimethylsulfonio)-5-oxo-L-norleucine bromide
-
-
2,3-dibromonaphthoquinone
-
0.015 mM, 41.5% inhibition
2-(tricyclo[3.3.1.13,7]dec-1-yl)ethyl prop-2-enoate
-
-
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
-
-
2-([3-(2-chlorophenyl)-4-oxo-5-phenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
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
-
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
-
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
-
-
2-([3-(3-fluorophenyl)-4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
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
-
-
2-([3-(3-fluorophenyl)-5-(2-hydroxyphenyl)-4-oxo-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-([3-(3-fluorophenyl)-5-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
-
2-([3-(3-fluorophenyl)-5-(3-diethylaminopropoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
-
2-([3-(3-fluorophenyl)-5-(3-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl]thio)acetohydrazide
-
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
-
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
-
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
-
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
-
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
-
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
-
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
-
50% inhibition at 0.0008 mM, standard format, at 0.00029 mM, full progress curve
2-aminonaphthoquinone
-
0.015 mM, 33.4% inhibition
2-Aminophenol
-
-
2-Aminothiophenol
-
-
2-bromo-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
-
-
2-bromo-3-hydroxynaphthoquinone
-
0.015 mM, 35.4% inhibition
2-chloro-1-(tricyclo[3.3.1.13,7]dec-1-yl)ethanone
-
-
2-Iodoacetamide
-
-
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 enzyme’s 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-Aminophenol
-
-
3-aminothiophenol
-
-
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-Aminophenol
-
-
4-aminothiophenol
-
-
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
butanolamine
-
-
Ca2+
-
above 10 mM
cadaverine
Ce3+
-
not reversible by Ca2+
chlorpromazine
Co2+
Nemipterus sp.
-
-
CP30a
reversible inhibitor
CP4d
reversible inhibitor
cystamine
cystamine dihydrochloride
-
1 mM and 10 mM for normal skin and keloid scar, respectively
cysteamine
-
50% inhibition at 0.178 mM
cysteine
-
85% inhibition
Dansylcadaverine
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)
ERW1041E
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
ethanolamine
-
-
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
-
-
Fe3+
strong inhibition
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
GTP-gamma-S
HgCl2
-
5 mM, 96% inhibition in the presence of 10 mM Ca2+
hydroxylamine
-
100 mM, complete inhibition
indirubin
-
-
iodoacetamide
iodoacetic acid
isatin
-
weak, reversible inhibitor
isoindigotin
-
-
K+
-
1 mM, 41% inhibition
KCC009
La3+
-
not reversible by Ca2+
LDN-27219
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 ketone
-
-
methyl N-[(benzyloxy)carbonyl]-L-phenylalanyl-6-(dimethylsulfonio)-5-oxo-L-norleucinate bromide
-
-
methyl N2-[(benzyloxy)carbonyl]-N6-(prop-2-enoyl)-L-lysylglycinate
-
-
methylamine
MgCl2
-
5 mM, 88% inhibition, 30% inhibition in the presence of 10 mM Ca2+
monodansyl cadaverine
Monodansylcadaverine
monoiodoacetate
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-(biotinyl)cadaverine
-
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-ethylmaleimide
N-iodoacetyl-N'-(5-sulfo-1-naphthyl)ethylenediamine
-
0.01 mM, 91% and 92% inhibition of chondrosarcoma transglutaminases B and C respectively
N-phenylacrylamide
-
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-toluyl]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
p-chloromercuribenzoate
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
propanolamine
-
-
putrescine
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
spermidine
spermine
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
ZnCl2
[(2-[[(benzyloxy)carbonyl]amino]-4-[5-(formylamino)-1,2,4-thiadiazol-3-yl]butanoyl)amino]acetic acid
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-
[(4-[3-(aminocarbonyl)oxiran-2-yl]-2-[[(benzyloxy)carbonyl]amino]butanoyl)amino]acetic acid
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[(5R,8S)-8-{[(benzyloxy)carbonyl]amino}-5-(methoxycarbonyl)-2,7-dioxo-9-phenylnonyl](dimethyl)sulfonium bromide
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[([3-(aminocarbonyl)oxiran-2-yl][[(benzyloxy)carbonyl]amino]acetyl)amino]acetic acid
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[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-ylmethyl]-carbamic acid benzyl ester
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[1-(4-acryloylaminobenzenesulfonyl)piperidin-4-yl]-carbamic acid benzyl ester
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[2-[(2-[4-[5-(dimethylamino)naphthalene-1-sulfonyl]piperazin-1-yl]-2-oxoethyl)amino]-2-oxoethyl](dimethyl)sulfanium
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[2-[(3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-2,3-dioxopropyl)amino]-2-oxoethyl](diethyl)sulfanium bromide
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[2-[(3-[4-[(benzyloxy)carbonyl]piperazin-1-yl]-2,3-dioxopropyl)amino]-2-oxoethyl](dimethyl)sulfanium bromide
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[2-[(4-acryloylaminobenzenesulfonyl)methylamino]ethyl]-methylcarbamic acid benzyl ester
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[4-(4-acryloylpiperazine-1-sulfonyl)phenyl]carbamic acid benzyl ester
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[4-[(4-aminophenyl)sulfonyl]piperazin-1-yl](cyclopropyl)methanone
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[[(4E)-6-amino-2-[[(benzyloxy)carbonyl]amino]-6-oxohex-4-enoyl]amino]acetic acid
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[[(5E)-7-amino-2-[[(benzyloxy)carbonyl]amino]-7-oxohept-5-enoyl]amino]acetic acid
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[[(6Z)-8-amino-2-[[(benzyloxy)carbonyl]amino]-8-oxooct-6-enoyl]amino]acetic acid
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additional information
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