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.

• Sinônimo(s): Cathepsin K Inhibitor I, 1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
• Fórmula empírica (Notação de Hill): C₃₁H₄₂N₄O₇
• Peso molecular: 582.69
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: lyophilized solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze
• cor: off-white
• solubilidade: methanol: 1 mg/mL; DMSO: soluble
• Condições de expedição: wet ice
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

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).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
cathepsin K

Product does not compete with ATP.

Reversible: yes

Target K_i: 22 nM against cathepsin K

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Sequência

Cbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable