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E-64

E-64

产品编号 T6037   CAS 66701-25-5
别名: Proteinase inhibitor E 64, E 64, E64

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 Chemical Structure
E-64, CAS 66701-25-5
规格 价格/CNY 货期 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 * 10 mM (in DMSO) ¥ 398 现货
产品目录号及名称: E-64 (T6037)
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生物活性
化学信息
存储 & 溶解度
参考文献
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 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 induces a marked decrease in the number of spontaneous metastasis in M5076 tumor bearing mice, while has no effect on the formation of experimental metastasis. [6] E-64 also shows antiparasitic activity against Giardia lamblia excystation in infected mice. [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

溶解度

H2O: 9 mg/mL (25.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 66 mg/mL (184.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.7979 mL 13.9895 mL 27.9791 mL 69.9477 mL
5 mM 0.5596 mL 2.7979 mL 5.5958 mL 13.9895 mL
10 mM 0.2798 mL 1.399 mL 2.7979 mL 6.9948 mL
20 mM 0.1399 mL 0.6995 mL 1.399 mL 3.4974 mL
DMSO 50 mM 0.056 mL 0.2798 mL 0.5596 mL 1.399 mL
100 mM 0.028 mL 0.1399 mL 0.2798 mL 0.6995 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Matsumoto K, et al. Biopolymers. 1999, 51(1), 99-107. 2. Barrett AJ, et al. Biochem J. 1982, 201(1), 189-198. 3. Kobayashi H, et al. Cancer Res. 1992, 52(13), 3610-3614. 4. Hussein EM, et al. J Egypt Soc Parasitol. 2009, 39(1), 111-119. 5. Min SH, et al. J Reprod Dev. 2014, 60(1), 21-27. 6. Blass G, et al. Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats. Physiol Rep. 2016 Sep;4(17). pii: e12950. 7. Zhang B, Chen Z. Screening of cathepsin B inhibitors in traditional Chinese medicine by capillary electrophoresis with immobilized enzyme microreactor[J]. Journal of Pharmaceutical and Biomedical Analysis. 2019: 112811. 8. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma[J]. Science Translational Medicine. 2020, 12(562).

文献引用

1. Guan X N, Zhang T, Yang T, et al. Covalent Sortase A Inhibitor ML346 Prevents Staphylococcus aureus Infection of Galleria mellonella. RSC Medicinal Chemistry. 2022 2. Jiang T Y, Pan Y F, Wan Z H, et al. PTEN status determines chemosensitivity to proteasome inhibition in cholangiocarcinoma. Science Translational Medicine. 2020, 12(562). 3. Zhang B, Chen Z. Screening of cathepsin B inhibitors in traditional Chinese medicine by capillary electrophoresis with immobilized enzyme microreactor. Journal of Pharmaceutical and Biomedical Analysis. 2019: 112811
Necrostatin-1 Vemurafenib Diosgenin glucoside Simvastatin Lomustine Isotretinoin Andrographolide Wogonoside

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 临床前化合物库 已知活性化合物库 经典已知活性库 抗菌活性库 NO PAINS 化合物库 抗感染化合物库 抗COVID-19化合物库 细胞凋亡化合物库 抗癌化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

E-64 66701-25-5 Autophagy Microbiology/Virology Proteases/Proteasome Cysteine Protease Antibacterial Proteinase inhibitor E 64 Cathepsin E 64 Inhibitor Proteinase inhibitor E-64 inhibit Proteinase inhibitor E64 E64 Bacterial inhibitor

 

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