Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary Targetµ-calpain

Cell permeable: yes

Target IC₅₀: 7.5 nM for µ-calpain and 78 nM for m-calpain; 15 nM and 1.6 nM against cathepsin B and L, respectively

General description

A potent, cell-permeable, reversible inhibitor of calpain (IC₅₀ = 7.5 nM for µ-calpain and 78 nM for m-calpain). Also potently inhibits cathepsin B (IC₅₀ = 15 nM) and L (IC₅₀ = 1.6 nM). Reduces bFGF-induced angiogenesis in rat cornea and prevents selenite cataract formation. Reduces A23187-induced nuclear opacity and proteolysis of crystallins and α-spectrin in cultured lenses.

A cell-permeable peptide aldehyde that acts as a potent and reversible inhibitor of calpain (IC₅₀ = 7.5 nM for µ-calpain and 78 nM for m-calpain). Also potently inhibits cathepsin B (IC₅₀ = 15 nM) and cathepsin L (IC₅₀ = 1.6 nM). Reduces βFGF-induced angiogenesis in rat cornea and prevents selenite cataract formation in rats. Reduces A23187-induced nuclear opacity and proteolysis of crystallins and α-spectrin in cultured rat lenses.

Legal Information

Sold under license of U.S. Patent 6,551,999

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Inoue, J., et al. 2003. J. Med. Chem.46, 868.Tamada, Y., et al. 2001. Curr. Eye Res.22, 280.Mathur, P., et al. 2000. Curr. Eye Res.21, 926.Nath, R., et al. 2000. Biochem. Biophys. Res. Commun.274, 16.Tamada, Y., et al. 2000. J. Ocul. Pharmacol. Ther.16, 271.Fukiage, C., et al. 1998. Curr. Eye Res.17, 623.Fukiage, C., et al. 1997. Biochim. Biophys. Acta 1361, 304.

Packaging

1, 5 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 3 months at -20°C.

Sequence

4-Fluorophenylsulfonyl-Val-Leu-CHO

Warning

Toxicity: Standard Handling (A)