Literature summary for 3.4.22.56 extracted from

Okun, I.; Malarchuk, S.; Dubrovskaya, E.; Khvat, A.; Tkachenko, S.; Kysil, V.; Ilyin, A.; Kravchenko, D.; Prossnitz, E.R.; Sklar, L.; Ivachtchenko, A.
Screening for caspase-3 inhibitors: a new class of potent small-molecule inhibitors of caspase-3 (2006), J. Biomol. Screen., 11, 277-285.

Search for more literature for 3.4.22.56

Activating Compound

Activating Compound	Comment	Organism	Structure
1,2-benzenedithiol	4-5fold activation	Homo sapiens
1,3-benzenedithiol	6fold activation	Homo sapiens
2-mercaptoethanol	half-maximal activation at 1.4 mM	Homo sapiens
4,4-thiobisbenzenethiol	4-5fold activation	Homo sapiens
dithiothreitol	half-maximal activation at 1.1 mM	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
1,2-butanedithiol	60% inhibition	Homo sapiens
1-methyl-5-[[(3R)-3-(phenoxymethyl)pyrrolidin-1-yl]sulfonyl]-1H-indole-2,3-dione	i.e. GSK-31, inhibitory effect is greatest in presence of 2-mercaptoethanol and decreases 2fold by substitution of 2-mercaptoethanol with dithiothreitol	Homo sapiens
2-(2-hydroxyethyl)-4-methyl-8-[(4-methylpiperidin-1-yl)sulfonyl]-1H-pyrrolo[3,4-c]quinoline-1,3(2H)-dione	i.e. CD-001-0011, 50% inhibition at 130 nM, reversible, inhibitory effect is greatest in presence of dithiothreitol and decreases 3-4fold by substitution of dithiothreitol with 2-mercaptoethanol	Homo sapiens
lipoic acid	80% inhibition	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
5.6	-	acetyl-DEVD-7-amido-4-methylcoumarin	pH 7.4, presence of 5 mM 2-mercaptoethanol	Homo sapiens
10.4	-	acetyl-DEVD-7-amido-4-methylcoumarin	pH 7.4, presence of 5 mM dithiothreitol	Homo sapiens
10.7	-	acetyl-DEVD-7-amido-4-methylcoumarin	pH 7.4	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	commercial preparation, recombinant full-length enzyme expressed in Escherichia coli	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
acetyl-DEVD-7-amido-4-methylcoumarin + H2O	-	Homo sapiens	acetyl-DEVD + 7-amino-4-methylcoumarin	-	?

Use of this online version of BRENDA is free under the CC BY 4.0 license. See terms of use for full details.

Release 2023.1 (January 2023)