219377

Cathepsin K Inhibitor I

The Cathepsin K Inhibitor I controls the biological activity of Cathepsin K. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• 別名: Cathepsin K Inhibitor I, 1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
• 実験式（ヒル表記法）: C₃₁H₄₂N₄O₇
• 分子量: 582.69
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: lyophilized solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: off-white
• 溶解性: methanol: 1 mg/mL; DMSO: soluble
• 輸送温度: wet ice
• 保管温度: −20°C

詳細

詳細

A cell-permeable, symmetrical bis(acylamino)ketone compound that acts as a potent, selective, reversible inhibitor of cathepsin K (K_i, = 22 nM). Also shown to inhibit cathepsin K in stably transfected CHO cells (IC₅₀ = 134 nM). Reported to bind to cathepsin K and span both the S- and S′- subsites. Inhibits papain (K_i >10 µM), trypsin (K_i >50 µM), and chymotrypsin (K_i >50 µM) only at higher concentrations. Exhibits greater selectivity for cysteine proteases of the papain family (K_i = 340 nM, 890 nM, and 1-3 µM for cathepsin L, cathepsin S, and cathepsin B, respectively).

A cell-permeable, symmetrical bis(acylamino)ketone that acts as a potent, selective, and reversible inhibitor of cathepsin K (K_i,app = 22 nM). Shown to bind to cathepsin K and span both the S- and S′-subsites. A poor inhibitor of papain (K_i,app >10 µM) but displays greater selectivity towards other proteases of the papain family (K_i,app = 340 nM, 890 nM, and 1.3 µM for cathepsin L, cathepsin S, and cathepsin B respectively). Inhibits trypsin and chymotrypsin activities only at higher concentrations (K_i,app ≥ 50 µM).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
cathepsin K

Product does not compete with ATP.

Reversible: yes

Target K_i: 22 nM against cathepsin K

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

シーケンス

Cbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz

再構成

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

その他情報

Claveau, D., et al. 2000. Biochem. Pharmacol.60, 759.
LaLonde, J.M., et al. 1999. Biochemistry38, 862.
Yamashita, D.S., et al. 1997. J. Am. Chem. Soc.119, 11351.

法的情報

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