Cathepsin K Inhibitor III

Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary TargetCathepsin K

Target K_i: 9.7 nM against cathepsin K

Cell permeable: yes

General description

A cell-permeable, potent, selective, reversible inhibitor of cathepsin K (K_i,app = 9.7 nM). At higher concentrations also inhibits the activities of cathepsin L, cathepsin B, and papain (K_i,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.

A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (K_i,app = 9.7 nM). At higher concentrations, also inhibits the activities of cathepsin L, cathepsin B, and papain (K_i,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.

Legal Information

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

Other Notes

Wang, D., et al. 2002. Biochemistry41, 8849.

Packaging

Packaged under inert gas

1 mg in Glass bottle

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

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

Sequence

H-Phe-Leu-NHNH-CO-NHNH-Leu-Z

Warning

Toxicity: Standard Handling (A)