VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.IC50 value: Target: 130/250/250/330/2.3/4.7 nM(Ki for cathepsin S/L/ZV/Bhumanized-rabbit cathepsin K/cathepsin F) [1]VBY-825 is a potent inhibitor of the assayed cathepsins and its potency against at least one cathepsin, cathepsin S, extends across species relevant for pharmacology studies, specifically mouse. 10 mg/kg/day dose of VBY-825 achieves a trough plasma concentration >200nM, which is well above that required for full inhibition of the intracellular activity of cathepsins B, F, K, L, S and V in both mouse and human cell lines.
[1]. Elie BT, et al. Identification and pre-clinical testing of a reversible cathepsin protease inhibitor reveals anti-tumor efficacy in a pancreatic cancer model. Biochimie. 2010 Nov;92(11):1618-24.