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Merck
CN

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.

别名:

Calpain Inhibitor VI, N-(4-Fluorophenylsulfonyl)-L-valyl-L-leucinal, SJA6017

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关于此项目

经验公式（希尔记法）:
C17H25FN2O4S
化学文摘社编号:
190274-53-4
分子量:
372.45
MDL number:
MFCD00954660
UNSPSC Code:
12352200
NACRES:
NA.77

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产品名称

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.

SMILES string

Fc1ccc(cc1)[S](=O)(=O)NC(C(C)C)C(=O)NC(CC(C)C)C=O

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

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

Quality Level

100

相关类别

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

Disclaimer

Toxicity: Standard Handling (A)

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.

Legal Information

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

Other Notes

4-Fluorophenylsulfonyl-Val-Leu-CHO
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

Packaged under inert gas

Preparation Note

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

存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

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