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
• 经验公式（希尔记法）: C₁₇H₂₅FN₂O₄S
• CAS号: 190274-53-4
• 分子量: 372.45
• MDL编号: MFCD00954660
• UNSPSC代码: 12352200
• NACRES: NA.77

属性

• 质量水平: 100
• 方案: ≥97% (HPLC)
• 表单: lyophilized solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; protect from light
• 颜色: white
• 溶解性: DMSO: 5 mg/mL
• 运输: ambient
• 储存温度: −20°C
• SMILES字符串: 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

说明

一般描述

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.

生化/生理作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

序列

4-Fluorophenylsulfonyl-Val-Leu-CHO

重悬

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

其他说明

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.

法律信息

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

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 1
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable