The Caspase-3/7 Inhibitor I, also referenced under CAS 220509-74-0, controls the biological activity of Caspase-3/7. This small molecule/inhibitor is primarily used for Cancer applications.
Synonym(s):
Caspase-3/7 Inhibitor I, 5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
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 µM). 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 µM). Also 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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target caspase-3
Product does not compete with ATP.
Reversible: yes
Target Ki: 60 nM, 170 nM, against caspase-3 and caspase-7, respectively
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Lee, D., et al. 2001. J. Med. Chem.44, 2015. Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
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