Merck, 219381-1MG, Cathepsin K Inhibitor III

General description
A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (Ki,app = 9.7 nM). At higher concentrations, also inhibits the activities of cathepsin L, cathepsin B, and papain (Ki,app = 120 nM, 5.1 µM, and 2.3 µM, respectively). Completely blocks cathepsin K activity in primary human synovial fibroblast cultures at 1 µM.
A cell-permeable, potent, selective, reversible inhibitor of cathepsin K (Ki,app = 9.7 nM). At higher concentrations also inhibits the activities of cathepsin L, cathepsin B, and papain (Ki,app = 120 nM, 5.1 mM, and 2.3 µM, respectively). Reported to completely block cathepsin K activity in primary human synovial fibroblast cultures at a concentration of 1 µM.
Biochem/physiol Actions
Target Ki: 9.7 nM against cathepsin K
Cell permeable: yes
Primary Target
Cathepsin K
Product does not compete with ATP.
Reversible: yes
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
H-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Wang, D., et al. 2002. Biochemistry41, 8849.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)