Calpain Inhibitor VI-CAS 190274-53-4-Calbiochem

C₁₇H₂₅FN₂O₄S

372.45

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.

Product does not compete with ATP.
Reversible: yes
Cell permeable: yes
Primary Target
µ-calpain
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

Toxicity: Standard Handling (A)

4-Fluorophenylsulfonyl-Val-Leu-CHO

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

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.

Sold under license of U.S. Patent 6,551,999
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

100

≥97% (HPLC)

lyophilized solid

Calbiochem^®

OK to freeze
protect from light

white

DMSO: 5 mg/mL

ambient

−20℃

1, 5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 1