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Literature summary for 3.4.22.56 extracted from

  • Han, Y.; Giroux, A.; Colucci, J.; Bayly, C.I.; Mckay, D.J.; Roy, S.; Xanthoudakis, S.; Vaillancourt, J.; Rasper, D.M.; Tam, J.; Tawa, P.; Nicholson, D.W.; Zamboni, R.J.
    Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors (2005), Bioorg. Med. Chem. Lett., 15, 1173-1180.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
(3R)-3-ethyl-1-[methyl(octyl)amino]-6-[3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]octane-2,5-dione 50% inhibition at 9 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells Homo sapiens
(3R)-3-ethyl-6-[2-oxo-3-[(1,3-thiazol-5-ylmethyl)amino]pyrazin-1(2H)-yl]-1-(phenylsulfanyl)octane-2,5-dione 50% inhibition at 12 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells Homo sapiens
(3R)-3-ethyl-6-[3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-1-(phenylsulfanyl)octane-2,5-dione 50% inhibition at 7.9 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells Homo sapiens
(3R)-3-ethyl-6-[5-ethyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-1-[hexyl(methyl)amino]octane-2,5-dione 50% inhibition at 6 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells Homo sapiens
(3R)-6-[5-tert-butyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-3-ethyl-1-[hexyl(methyl)amino]octane-2,5-dione i.e. M826, 50% inhibition at 6 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells Homo sapiens
(3R)-6-[5-tert-butyl-3-[[(4-methyl-1,2,5-oxadiazol-3-yl)methyl]amino]-2-oxopyrazin-1(2H)-yl]-3-ethyl-1-[methyl(pentyl)amino]octane-2,5-dione i.e. M867, 50% inhibition at 0.1 nM, reversible. Comparison with inhibition of caspase-1, caspase-7, caspase-8 and NT2 whole cells Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 recombinant enzyme
-