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Literature summary for 3.4.22.56 extracted from

  • Vickers, C.J.; Gonzalez-Paez, G.E.; Wolan, D.W.
    Selective detection and inhibition of active caspase-3 in cells with optimized peptides (2013), J. Am. Chem. Soc., 135, 12869-12876.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
Ac-CV3-KE
-
Homo sapiens
Ac-DW3-KE
-
Homo sapiens
Ac-F-D-beta-hLeu-hLeu-D-KE
-
Homo sapiens
FAM-Ahx2-CV3-AOMK
-
Homo sapiens
FAM-DEVD-AOMK
-
Homo sapiens
methyl N-acetyl-3-(pyridin-3-yl)-D-alanyl-N-[[(3S)-1-[(2R)-1-[(3S)-1-methoxy-5-[[(5-methylthiophen-2-yl)carbonyl]oxy]-1,4-dioxopentan-3-yl]amino-1-oxo-3-phenylpropan-2-yl]amino]-5-methyl-1-oxohexan-3-yl]-L-alpha-asparaginate low nanomolar potency against caspase-3 with more than 120fold selectivity over caspase-7 Homo sapiens
N-acetyl-3-(pyridin-3-yl)-L-alanyl-N-[(3S)-1-[[(2S)-1-([(2S)-1-carboxy-4-[(2,6-dimethylbenzoyl)oxy]-3-oxobutan-2-yl]amino)-5-methyl-1-oxohexan-2-yl]amino]-5-methyl-1-oxohexan-3-yl]-L-alpha-asparagine low nanomolar potency against caspase-3 with more than 30fold selectivity over caspase-7 Homo sapiens
Rho-DEVD-AOMK
-
Homo sapiens
Z-VAD-fluoromethylketone
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HeLa cell
-
Homo sapiens
-

Substrates and Products (Substrate)

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000068
-
at pH 7.4 and 22°C Homo sapiens Ac-CV3-KE
0.00001
-
at pH 7.4 and 22°C Homo sapiens Rho-DEVD-AOMK
0.000012
-
at pH 7.4 and 22°C Homo sapiens Ac-F-D-beta-hLeu-hLeu-D-KE
0.000018
-
at pH 7.4 and 22°C Homo sapiens FAM-DEVD-AOMK
0.000023
-
at pH 7.4 and 22°C Homo sapiens N-acetyl-3-(pyridin-3-yl)-L-alanyl-N-[(3S)-1-[[(2S)-1-([(2S)-1-carboxy-4-[(2,6-dimethylbenzoyl)oxy]-3-oxobutan-2-yl]amino)-5-methyl-1-oxohexan-2-yl]amino]-5-methyl-1-oxohexan-3-yl]-L-alpha-asparagine
0.000027
-
at pH 7.4 and 22°C Homo sapiens FAM-Ahx2-CV3-AOMK
0.01
-
at pH 7.4 and 22°C Homo sapiens Ac-DW3-KE