190274-53-4

Calpain inhibitor VI is an inhibitor of the calcium-dependent cysteine proteases μ-calpain (calpain-1; IC₅₀ = 7.5 nM) and m-calpain (calpain-2; IC₅₀ = 78 nM). It also inhibits cathepsins B and L (IC₅₀s = 15 and 1.6 nM, respectively). It is selective for these calpains and cathepsins over other cysteine and serine proteases, factor VIIa, factor Xa, trypsin, chymotrypsin, and proteasome. In an in vitro porcine model of cataract, calpain inhibitor VI decreases the degree of cataract by 40% when used at a concentration of 0.8 μM. It also prevents cataract formation induced by selenite in rats when administered at a dose of 100 mg/kg for 4 days. Calpain inhibitor VI improves functional outcome and reduces apoptotic cell death in a rat model of spinal cord injury.

Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract[1].

[1] C Fukiage, et al. SJA6017, a newly synthesized peptide aldehyde inhibitor of calpain: amelioration of cataract in cultured rat lenses. Biochim Biophys Acta. 1997 Oct 24;1361(3):304-12. DOI:10.1016/s0925-4439(97)00043-4