General description
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
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
5-[(S)-(+)-2-(Methoxymethyl)pyrrolidino]sulfonylisatin
Reconstitution
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
- UPC:
- 51283102
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 218826-1MG
