Merck, 219379-1MG, Cathepsin K Inhibitor II

General description
A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (Ki = 6 nM). Reported to completely block cathepsin K activity in primary human synovial fibroblast cultures at a concentration of 1 µM. Also shown to inhibit the activity of cathepsin B and papain at higher concentrations (Ki = 510 nM and 1.2 µM, respectively). Does not significantly inhibit cathepsin L.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
cathepsin K
Product does not compete with ATP.
Reversible: yes
Target Ki: 6 nM against cathepsin; 510 nM, 1.2 µM, against cathepsin B and papain, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Boc-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)