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Literature summary 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.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.22.56 1,2-benzenedithiol 4-5fold activation Homo sapiens
3.4.22.56 1,3-benzenedithiol 6fold activation Homo sapiens
3.4.22.56 2-mercaptoethanol half-maximal activation at 1.4 mM Homo sapiens
3.4.22.56 4,4-thiobisbenzenethiol 4-5fold activation Homo sapiens
3.4.22.56 dithiothreitol half-maximal activation at 1.1 mM Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.56 1,2-butanedithiol 60% inhibition Homo sapiens
3.4.22.56 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
3.4.22.56 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
3.4.22.56 lipoic acid 80% inhibition Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.22.56 5.6
-
 acetyl-DEVD-7-amido-4-methylcoumarin pH 7.4, presence of 5 mM 2-mercaptoethanol Homo sapiens
3.4.22.56 10.4
-
 acetyl-DEVD-7-amido-4-methylcoumarin pH 7.4, presence of 5 mM dithiothreitol Homo sapiens
3.4.22.56 10.7
-
 acetyl-DEVD-7-amido-4-methylcoumarin pH 7.4 Homo sapiens

Organism

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

Substrates and Products (Substrate)

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