| 货号 | 10007963-1mg |
| 描述 | E-64 is a natural, potent, and irreversible inhibitor of cysteine proteases.1 Its IC50 values for inhibiting cathepsins K, S, and L, in vitro, are 1.4, 4.1, and 2.5 nM, respectively.2 E-64 also inhibits papain, calpain, and cathepsins B and H, but not serine proteases (e.g., plasmin, trypsin, tissue kallikrein) or aspartic proteases (e.g.,pepsin).3 The mode of action involves the formation of a thioether linkage between E-64 and the thiol group of the protease; E-64 does not react with the functional thiol group of non-protease enzymes (e.g., creatine kinase, L-lactate hydrogenase). While E-64 is usually used in biochemical assays, it can also be used in intact cells at higher (μM) concentrations.4,5,6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Drahl, C.,Cravatt, B.F., and Sorensen, E.J. Protein-reactive natural products. Angewandte Chemie International Edition 44, 5788-5809 (2005). 2.Susa, M.,Luong-Nguyen, N.H.,Cappellen, D., et al. Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay. Journal of Translational Medicine 2(6), (2004). 3.Barrett, A.J.,Kembhavi, A.A.,Brown, M.A., et al. L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L. Biochemistry Journal 201, 189-198 (1982). 4.Giusti, I.,DAscenzo, S.,Millimaggi, D., et al. Cathepsin B mediates the pH-dependent proinvasive activity of tumor-shed microvesicles. Neoplasia 10(5), 481-488 (2008). 5.Ahlberg, J.,Berkenstam, A.,Henell, F., et al. Degradation of short and long lived proteins in isolated rat liver lysosomes; effects of pH, temperature, and proteolytic inhibitors. The Journal of Biological Chemisty 260(9), 5847-5854 (1985). 6.Drew, M.E.,Banerjee, R.,Uffman, E.W., et al. Plasmodium food vacuole plasmepsins are activated by falcipains. The Journal of Biological Chemisty 283(19), 12870-12876 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 357.41 |
| 分子式 | C15H27N5O5 |
| CAS号 | 66701-25-5 |
| 稳定性 | ≥ 2 years |
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