103476-89-7Leupeptin, Microbial

产品属性：

Cas No.103476-89-7

别名 Leupeptin hemisulfate salt microbial,L-Leucinamide,Leupeptin, Microbial

化学名 2-acetamido-N-(1-((5-((diaminomethylene)amino)-1-oxopentan-2-yl)amino)-4-methyl-1-oxopentan-2-yl)-4-methylpentanamide

分子式 C20H38N6O4.1/2H2SO4

分子量 493.6

溶解度 ≥ 24.7mg/mL in DMSO， ≥ 20mg/mL in Water

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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].

References:

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.