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Literature summary for 3.4.22.1 extracted from

  • Wisastra, R.; Ghizzoni, M.; Maarsingh, H.; Minnaard, A.J.; Haisma, H.J.; Dekker, F.J.
    Isothiazolones; thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF (2011), Org. Biomol. Chem., 9, 1817-1822.
    View publication on PubMed
Search for more literature for 3.4.22.1

Inhibitors

Inhibitors Comment Organism Structure
2-(3-chloro-4-fluorophenyl)-1,2-thiazol-3(2H)-one
-
 Homo sapiens
2-pentyl-1,2-thiazol-3(2H)-one
-
 Homo sapiens
2-phenylisothiazol-3(2H)-one
-
 Homo sapiens
5-chloro-2-(2-chloro-4,5-dimethoxyphenethyl)isothiazol-3(2H)-one
-
 Homo sapiens
5-chloro-2-(3-chloro-4-fluorophenyl)-1,2-thiazol-3(2H)-one
-
 Homo sapiens
5-chloro-2-pentyl-1,2-thiazol-3(2H)-one
-
 Homo sapiens
5-chloro-2-phenylisothiazol-3(2H)-one
-
 Homo sapiens
ethyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
 Homo sapiens
methyl 3-(4,5-dichloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
 Homo sapiens
methyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
 Homo sapiens
methyl 3-(5-chloro-4-methyl-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
-
 Homo sapiens
methyl 4-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)butanoate
-
 Homo sapiens
methyl 6-(3-(propyldisulfanyl)acrylamido)hexanoate
-
 Homo sapiens
N-phenyl-3-(propyldisulfanyl)-3-chloro-acrylamide
-
 Homo sapiens
N-phenyl-3-(propyldisulfanyl)acrylamide
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
1.2
-
 Cbz-L-Arg-L-Arg-7-amido-4-trifluoromethylcoumarin in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Cbz-L-Arg-L-Arg-7-amido-4-trifluoromethylcoumarin + H2O
-
 Homo sapiens Cbz-L-Arg-L-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
CatB
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000046
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens N-phenyl-3-(propyldisulfanyl)-3-chloro-acrylamide
0.0041
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 5-chloro-2-(2-chloro-4,5-dimethoxyphenethyl)isothiazol-3(2H)-one
0.0073
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 5-chloro-2-pentyl-1,2-thiazol-3(2H)-one
0.0085
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens methyl 3-(4,5-dichloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
0.011
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens methyl 3-(5-chloro-4-methyl-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
0.011
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens methyl 4-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)butanoate
0.012
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens methyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
0.012
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens N-phenyl-3-(propyldisulfanyl)acrylamide
0.013
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 2-pentyl-1,2-thiazol-3(2H)-one
0.013
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 5-chloro-2-phenylisothiazol-3(2H)-one
0.014
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens ethyl 3-(5-chloro-3-oxo-1,2-thiazol-2(3H)-yl)propanoate
0.024
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens methyl 6-(3-(propyldisulfanyl)acrylamido)hexanoate
0.042
-
 in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 5-chloro-2-(3-chloro-4-fluorophenyl)-1,2-thiazol-3(2H)-one
0.1
-
 IC50 above 0.1 mM, in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 2-phenylisothiazol-3(2H)-one
0.1
-
 IC50 above 0.1 mM, in 100 mM Na2HPO4, 1.25 mM EDTA., pH 6.8, at 25°C Homo sapiens 2-(3-chloro-4-fluorophenyl)-1,2-thiazol-3(2H)-one