Calpain Inhibitor VI

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).¹ 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.² It also prevents cataract formation induced by selenite in rats when administered at a dose of 100 mg/kg for 4 days.³ Calpain inhibitor VI improves functional outcome and reduces apoptotic cell death in a rat model of spinal cord injury.⁴

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1. Inoue, J., Nakamura, M., Cui, Y.-S., et al. Structure-activity relationship study and drug profile of N-(4-fluorophenylsulfonyl)-L-valyl-L-leucinal (SJA6017) as a potent calpain inhibitor. J. Med. Chem. 46(5), 868-871 (2003).

2. Biswas, S., Harris, F., Singh, J., et al. The in vitro retardation of porcine cataractogenesis by the calpain inhibitor, SJA6017. Mol. Cell Biochem. 261(1-2), 169-173 (2004).

3. Tamada, Y., Fukiage, C., Mizutani, K., et al. Calpain inhibitor, SJA6017, reduces the rate of formation of selenite cataract in rats. Curr. Eye Res. 22(4), 280-285 (2001).

4. Akdemir, O., Uçankale, M., Karaoğlan, A., et al. Therapeutic efficacy of SJA6017, a calpain inhibitor, in rat spinal cord injury. J. Clin. Neurosci. 15(10), 1130-1136 (2008).