Caspase-3/7 Inhibitor I

Catalog #: 27741-1
Size: 5 mg
$305
MW: 324.4 Da
CAS Registry #: 220509-74-0
Formula: C14H16N2O5S
Target: Caspase3, 7
Background:
Selectivity for caspases-3 and 7 involves unique hydrophobic residues in the S2 pocket surrounding the catalytic cysteine residue. Sequence alignments of the active site residues of the caspases strongly suggest that the basis of this selectivity is due to binding in the S2 subsite comprised of residues Tyr204, Trp206, and Phe256 which are unique to caspases 3 and 7. In some systems inhibition of caspases-3 and -7 can prevent apoptosis and may therefore have important therapeutic implications.
Description:
A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.
Synonym(s):
Isatin Sulfonamide; 5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione
Biological Activity:
Caspase-3/7 inbibitor I is a potent, reversible, isatin sulfonamide-based inhibitor of caspase-3 (Ki = 60 nM, IC50= 120 nM) and caspase-7 (Ki = 170 nM). It is a weaker inhibitor of caspase-9 (Ki = 3.1 µM). It Has only a trivial effect (Ki(app) >25 µM) 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).
Solubility:
Soluble in DMSO
Format:
crystalline solid.
Storage / Stability:

Store at or below –20°C. Solid form is stable at least 12 months from date of receipt, when stored as directed. Do not store aqueous solutions for more than one day.

Reference(s):
1. Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
2. Lee, D., et al. 2001. J. Med. Chem. 44, 2015.
3. Dang, Q., et al. 2014. Molec. Carcinogenesis (ahead of print)
Scientific Category:
Apoptosis Inhibitor
Product Type:
Inhibitor
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