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Literature summary for 3.4.22.56 extracted from

  • Han, B.H.; Xu, D.; Choi, J.; Han, Y.; Xanthoudakis, S.; Roy, S.; Tam, J.; Vaillancourt, J.; Colucci, J.; Siman, R.; Giroux, A.; Robertson, G.S.; Zamboni, R.; Nicholson, D.W.; Holtzman, D.M.
    Selective, reversible caspase-3 inhibitor is neuroprotective and reveals distinct pathways of cell death after neonatal hypoxic-ischemic brain injury (2002), J. Biol. Chem., 277, 30128-30136.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
M826 IC50: 0.00003 mM; i.e. (R,S)-[[(2S)-2-[5-tert-butyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]butanoyl]amino]-5-[hexyl(methyl)amino]-4-oxopentanoic acid hydrochloride, selectively and potently inhibits both caspase-3 enzymatic activity and apoptosis in cultured cell in vitro Homo sapiens
M826 IC50 for enzyme from cerebellar granule neuron: 0.00005 mM. IC50 for enzyme from cortical neuron: 0.00012 mM; i.e. (R,S)-[[(2S)-2-[5-tert-butyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]butanoyl]amino]-5-[hexyl(methyl)amino]-4-oxopentanoic acid hydrochloride, selectively and potently inhibits both caspase-3 enzymatic activity and apoptosis in cultured cell in vitro Mus musculus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
cerebellum
-
 Mus musculus
-
neuron
-
 Mus musculus
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teratocarcinoma cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00003
-
 IC50: 0.00003 mM Homo sapiens M826
0.00012
-
 IC50 for enzyme from cerebellar granule neuron: 0.00005 mM. IC50 for enzyme from cortical neuron: 0.00012 mM Mus musculus M826