Caspase-3/7 Inhibitor I

Short Summary : Caspase-3/7 inhibitor

Category : Apoptosis|Caspase

Purity : 0.9723

CAS Number : 220509-74-0

Formula : C14H16N2O5S

Molecular Weight : 324.4

SMILE : COCC1CCCN1S(=O)(=O)C2=CC3=C(C=C2)NC(=O)C3=O

Solubility : >16.2mg/mL in DMSO

Storage : Store at -20°C

Description : 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., BurtonWurster, N., Nuttall, M. E., & Lust, G. (2005). Caspase3/7 inhibition alters cell morphology in mitomycinc treated chondrocytes. Journal of cellular physiology, 205(1), 133-140.

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