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Beschreibung

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (Ki = 60 nM) and caspase-7 (Ki = 170 nM)., A potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (KI(app) = 60 nM) and caspase-7 (KI(app) = 170 nM). Inhibits caspase-9 to a lesser extent (Ki(app) = 3.1 µ,M). Has only a trivial effect (Ki(app) >25 mM) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. Reported to inhibit apoptosis in camptothecin treated Jurkat cells (IC50 ~50 µ,M). Also reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 µ,M and 98% inhibition at 50 µ,M). Selectivity for caspases 3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue.