Biological Activity
caspase-3/7 inbibitor i is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (ki(app) = 60 nm) and caspase-7 (ki(app) = 170 nm). is a weaker inhibitor of caspase-9 (ki(app) = 3.1 mm). it has only a trivial effect (ki(app) >25 mm) on the activities of caspase-1, caspase-2, caspase-4, caspase-6, and caspase-8. it has been shown to inhibit apoptosis in camptothecin treated jurkat cells (ic50 ~50 μm). also it has been reported to inhibit apoptosis in chondrocytes (44% inhibition at 10 μm and 98% inhibition at 50 μm). selectivity for caspases-3 and 7 involves unique hydrophobic residues in the s2 pocket surrounding the catalytic cysteine residue. [1] [2] in some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications. [3]a potent, cell-permeable, and specific, reversible inhibitor of caspase-3 (ki = 60 nm) and caspase-7 (ki = 170 nm).
References
1. lee, d., et al. 2001. j. med. chem. 44, 2015. 2. lee, d., et al. 2000. j. biol. chem. 275, 16007. 3. clements, k. m., burton‐wurster, n., nuttall, m. e., & lust, g. (2005). caspase‐3/7 inhibition alters cell morphology in mitomycin?\c treated chondrocytes. journal of cellular physiology, 205(1), 133-140.
