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.

• 別名: Calpain Inhibitor VI, N-(4-Fluorophenylsulfonyl)-L-valyl-L-leucinal, SJA6017
• 実験式（ヒル表記法）: C₁₇H₂₅FN₂O₄S
• CAS番号: 190274-53-4
• 分子量: 372.45
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥97% (HPLC)
• フォーム: lyophilized solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: −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

詳細

詳細

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.

生物化学的／生理学的作用

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)

シーケンス

4-Fluorophenylsulfonyl-Val-Leu-CHO

再構成

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

その他情報

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.

法的情報

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

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable