Caspase-3/7 Inhibitor I

Catalog #

27741-2

$455 *

Size: 10 mg

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Description

A potent, cell-permeable, and specific, reversible inhibitor of caspase-3 and caspase-7.

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Synonyms

Isatin Sulfonamide; 5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]sulfonyl-1H-indole-2,3-dione, Caspase

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Product Info

Storage and Usage

Citations

Format

crystalline solid.

Target(s)

Caspase3, 7

Formula

C₁₄H₁₆N₂O₅S

324.4 Da

Solubility

Soluble in DMSO

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).

CAS Registry #

220509-74-0

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.

References

1. Lee, D., et al. 2000. J. Biol. Chem. 275, 16007.
2. Lee, D., et al. 2001. J. Med. Chem. 44, 2015.
3. Jiang Y., Hansen T.V. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1626-9.

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Caspase-3/7 Inhibitor I

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