208745

Calpain Inhibitor VI

The Calpain Inhibitor VI, also referenced under CAS 190274-53-4, controls the biological activity of Calpain. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): Calpain Inhibitor VI, N-(4-Fluorophenylsulfonyl)-L-valyl-L-leucinal, SJA6017
• Empirical Formula (Hill Notation): C₁₇H₂₅FN₂O₄S
• CAS Number: 190274-53-4
• Molecular Weight: 372.45
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥97% (HPLC)
• form: lyophilized solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 5 mg/mL
• shipped in: ambient
• storage temp.: −20°C
• InChI: 1S/C17H25FN2O4S/c1-11(2)9-14(10-21)19-17(22)16(12(3)4)20-25(23,24)15-7-5-13(18)6-8-15/h5-8,10-12,14,16,20H,9H2,1-4H3,(H,19,22)
• InChI key: WSJWUIDLGZAXID-UHFFFAOYSA-N

Description

General description

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.

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
µ-calpain

Product does not compete with ATP.

Reversible: 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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

4-Fluorophenylsulfonyl-Val-Leu-CHO

Reconstitution

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

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.

Legal Information

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

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable