CAS:66701-25-5E-64

E-64 is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

66701-25-5

储存条件

分子式

C15H27N5O5

运输

蓝冰

分子量

357.40

别名

溶解度

动物实验配方

生物活性

描述E 64 is a potent, irreversible, selective and water-soluble cysteine protease inhibitor with IC50 values of 1.4, 2.5 and 4.1 nM for cathepsin K, L and S, respectively, as well as exhibited inhibitory effect on papain, calpain, cathepsin B and cathepsin H, but not serine proteases (except trypsin)^[1]^[2]^[3]. E 64 had no effect on the serine proteinases at a concentration of 0.5 mM, but could inhibit the serine proteinases trypsin^[3]. Treatment with E 64 combined with pepstatin A could increase LC3-II accumulation due to the endogenous FoxO1 required autophagy induced by stress stimuli (oxidative stress or serum starvation)^[4]. Through inhibition of cathepsins (lysosomal proteases), E 64 is used as lysosomal protease inhibitor^[4]^[5]. E 64 is a main component of commercial used proteasome cocktail.
作用机制The epoxysuccinyl group of E-64 irreversibly binds with an active thiol group of cysteine proteases to form a thioether linkage.^[6]
动物研究
剂量
Mice: 1 mg/kg^[7] (i.p.)

给药途径
i.p.