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.

• Synonyme(s) : Cathepsin K Inhibitor I, 1,3-Bis(CBZ-Leu-NH)-2-propanone, 1,3-Bis(N-carbobenzoyloxy-L-leucyl)amino Acetone
• Formule empirique (notation de Hill): C₃₁H₄₂N₄O₇
• Poids moléculaire : 582.69
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥95% (HPLC)
• Forme: lyophilized solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: off-white
• Solubilité: methanol: 1 mg/mL; DMSO: soluble
• Conditions d'expédition: wet ice
• Température de stockage: −20°C

Description

Description générale

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).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
cathepsin K

Product does not compete with ATP.

Reversible: yes

Target K_i: 22 nM against cathepsin K

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Séquence

Cbz-Leu-NH-CH₂-CO-CH₂-NH-Leu-Cbz

Reconstitution

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

Autres remarques

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.

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 1
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable