化合物E64 T6037

Product Introduction
Bioactivity


英文名: E-64

描述: E-64 (Proteinase inhibitor E 64)是一种不可逆的半胱氨酸蛋白酶抑制剂，抑制papain 的IC50为 9 nM。

激酶实验: The Cathepsin Β activity is determined using Z-Arg-Arg-4mβNA as substrate with slight modifications. The crude extract is pre-incubated at 37°C for 5 min in 50 mM sodium acetate buffer, pH 5.0 containing 1 mM EDTA and 5 mM DTT. The substrate (final concentration, 100 μM) is added to make the final assay volume of 1 mL. The reaction mixture is incubated at 37°C for 30 min. The reaction is terminated by adding equal volume of stopping reagent containing Fast Garnet GBC salt (1 mg/mL), 10 mM pHMB and 50 mM EDTA, pH 6.0. The extraction of product, β-napthylamine (β-NA), is carried out with n-butanol. After complete layer separation, the absorbance is measured in n-butanol layer and activity is calculated using molar extinction coefficient of β-napthylamine solution as 31.5 M/cm per sec at 520 nm. One unit of enzyme activity is defined as the amount of enzyme liberating 1 μmol of βNA per minute at 37°C. The half maximal inhibitory concentration (IC50) is calculated by plotting the graph between the different concentration of E-64 and the % inhibition in cathepsin B activity. Here, IC50 indicates the concentration of the E-64 required to inhibit the parasitic cathepsin B activity by half[2].

体外活性: E-64 rapidly inhibits the activities of the cysteine proteinases cathepsins B, H and L and papain, while has no effect on the serine proteinases or the metalloproteinases. [2] E-64, as a specific inhibitor os cysteine proteases, effectively blocks in vitro ovarian cancer cell invasion. [3] In addition, E-64 also shows antiparasitic activity against Giardia lamblia excystation in vitro. [4] E-64 improves the preimplantation development of bovine somatic cell nuclear transfer embryos, which indicates another important implication of E-64. [5]

体内活性: E-64显著减少了携带M5076肿瘤的小鼠中自发性转移的数量，但对实验性转移的形成无影响。[6] E-64还对感染小鼠中的贾第鞭毛虫(excystation)表现出抗寄生虫活性。[4]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 9 mg/mL (25.2 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 50 mg/mL (139.9 mM)


关键字: Cathepsin | Inhibitor | Proteinase inhibitor E-64 | inhibit | Proteinase inhibitor E64 | E-64 | Bacterial | Autophagy

相关产品: ONO-5334 | KGP94 | SID 26681509 | MK-0674 | Odanacatib | N-Ethylmaleimide | Aureusimine B | (RS)-Butyryltimolol | E 64c | K777

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Autophagy Compound Library | Anti-Bacterial Compound Library | Preclinical Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途