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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 219 | 现货 | |
5 mg | ¥ 395 | 现货 | |
10 mg | ¥ 617 | 现货 | |
25 mg | ¥ 1,090 | 现货 | |
50 mg | ¥ 1,650 | 现货 | |
100 mg | ¥ 2,460 | 现货 | |
500 mg | ¥ 5,820 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | E-64 (Proteinase inhibitor E 64) is an irreversible and specific cysteine protease inhibitor. The IC50 of E-64 for papain is 9 nM. |
靶点活性 | Cysteine protease:9 nM |
体外活性 | E-64迅速抑制半胱氨酸蛋白酶如cathepsins B、H、L以及papain的活性,但对丝氨酸蛋白酶或金属蛋白酶无影响。[2]作为特异性半胱氨酸蛋白酶抑制剂,E-64有效阻止体外卵巢癌细胞侵袭。[3]此外,E-64还展现了针对体外Giardia lamblia excystation的抗寄生虫活性。[4]E-64改善牛体细胞核移植胚胎的种植前发展,这表明了E-64的另一个重要作用。[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] |
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]. |
别名 | Proteinase inhibitor E 64, E 64, E64 |
分子量 | 357.41 |
分子式 | C15H27N5O5 |
CAS No. | 66701-25-5 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 9 mg/mL (25.2 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (139.9 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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