E-64蛋白酶抑制剂

基本信息

英文名：E-64

别名：trans-Epoxysuccinyl-L-leucylamido(4-guanidino)butane;N-(trans-Epoxysuccinyl)-L-leucine 4-guanidinobutylamide

产品名称：N-(反式-环氧丁二酰基)-L-亮氨酸-4-胍基丁基酰胺

分子式：C₁₅H₂₇N₅O₅

分子量：357.41

CAS 登录号：66701-25-5

产品描述：

Preparation Note：

E-64 is soluble in water. A 20 mg/ml solution can be prepared in water (heat may be needed). A suggested stock solution is a 1 mM aqueous solution. The effective concentration for use as a protease inhibitor is 1 to10 μM. Aqueous stock solutions are stable for months at -20 °C. Diluted solutions are stable for days at neutral pH. E-64 is stable from pH 2-10, but is unstable in ammonia or in HCl. E-64 is also soluble in DMSO, a 10 mM solution can be prepared in dry DMSO and stored at -20 °C. Subsequent dilutions were in culture medium. Solutions for injection were prepared by dissolving E-64 in 0.9% sodium chloride or in a minimum amount of saturated sodium bicarbonate followed by dilution with 0.9% sodium chloride (after adjusting the pH to 7.0 with acetic acid).

Biochem/physiol Actions：

E-64 is an irreversible, potent, and highly selective cysteine protease inhibitor. E-64 does not react with the functional thiol group of non-protease enzymes, such as L-lactate dehydrogenase or creatine kinase. E-64 will not inhibit serine proteases (except trypsin) like other cysteine protease inhibitors, leupeptin and antipain. The trans-epoxysuccinyl group (active moiety) of E-64 irreversibly binds to an active thiol group in many cysteine proteases, such as papain, actinidase, and cathepsins B, H, and L to form a thioether linkage. E-64 is a very useful cysteine protease inhibitor for use in in vivo studies because it has a specific inhibition, it is permeable in cells and tissues and has low toxicity.

Solubility:H₂O: soluble1 mM (Stock Solutions stable for months at –20° C.)

storage temp:2-8°

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