CA-074

CA-074 is an epoxysuccinyl peptide inhibitor of cathepsin B. It selectively inhibits cathepsin B with an IC₅₀ of 2.24 nM over other cysteine proteinases such as cathepsins L and H, and calpains. It inhibits cathepsins H, L and calpain with IC₅₀ values of 172 μM, 420 μM and 200 μM. Intraperitoneal administration (50 mg/kg) of CA-074 reduces metastasis in 4T1.2 mouse xenograft model. It reduces mercury induced expression of inflammatory cytokines in mice.