Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary Targetcathepsin K

Target K_i: 6 nM against cathepsin; 510 nM, 1.2 µM, against cathepsin B and papain, respectively

Cell permeable: yes

General description

A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (K_i,app = 6 nM). Shown to completely block cathepsin K activity in primary human synovial fibroblast cultures at 1 µM. At higher concentrations, also inhibits the activities of cathepsin B and papain (K_i,app = 510 nM, 1.2 µM, respectively). Does not significantly inhibit cathepsin L.

A cell-permeable peptidyl bis-carbohydrazide compound that acts as a potent, selective, and reversible inhibitor of cathepsin K (K_i = 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 (K_i = 510 nM and 1.2 µM, respectively). Does not significantly inhibit cathepsin L.

Legal Information

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

Other Notes

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

Packaging

1 mg in Plastic ampoule

Packaged under inert gas

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Sequence

Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z

Warning

Toxicity: Standard Handling (A)