Inhibitor of serine and cysteine proteases
CAS：103476-89-7
分子式：C20H38N6O4.1/2H2SO4
分子量：493.6
纯度：98%
存储：Store at -20°C

Background:

Leupeptin is a reversible inhibitor of protease with Ki values of 35 nM, 3.4 μM, 6 nM and 72 nM for bovine trypsin, human plasmin, bovine spleen cathepsin B and recombinant human calpain, respectively [1, 2].

As a protease inhibitor, leupeptin was originally isolated from the Streptomyces species. It exerted poor membrane permeability due to its polar C-terminal. For calpain, leupeptin showed moderate potent activities with IC50 values of 0.211 μM, 1.8 μM and 0.938 μM against the enzymes isolated from porcine erythrocyte, porcine kidney and human platelet, respectively. In cultured MRC-C cells, leupeptin suppressed the growth of human coronavirus strain 229E through inhibited the activity of trypsin. The mean IC50 value was 0.8 μM [2, 3].

参考文献:
1.  Mehdi S. Cell-penetrating inhibitors of calpain. Trends in biochemical sciences, 1991, 16: 150-153.
2.  Krauser J A, Powers J C. 6.1 BIOLOGICAL ROLES. Proteinase and Peptidase Inhibition: Recent Potential Targets for Drug Development, 2003: 144.
3.  Appleyard G, Tisdale M. Inhibition of the growth of human coronavirus 229E by leupeptin. Journal of general virology, 1985, 66(2): 363-366.