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E-64

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Chemical Structure| 66701-25-5 同义名 : Proteinase inhibitor E 64
CAS号 : 66701-25-5
货号 : A252147
分子式 : C15H27N5O5
纯度 : 99%+
分子量 : 357.405
MDL号 : MFCD00080261
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(167.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(13.99 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • Cysteine Protease

    Cysteine protease, IC50:9 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

13.99mL

2.80mL

1.40mL

27.98mL

5.60mL

2.80mL
参考文献

[1]Susa M, Luong-Nguyen NH, et al. Human primary osteoclasts: in vitro generation and applications as pharmacological and clinical assay. J Transl Med. 2004 Mar 16;2(1):6.

[2]Murata M, Miyashita S, et al. Novel epoxysuccinyl peptides. Selective inhibitors of cathepsin B, in vitro. FEBS Lett. 1991 Mar 25;280(2):307-10.

[3]Barrett AJ, Kembhavi AA, et al. L-trans-Epoxysuccinyl-leucylamido(4-guanidino)butane (E-64) and its analogues as inhibitors of cysteine proteinases including cathepsins B, H and L. Biochem J. 1982 Jan 1;201(1):189-98.

[4]Zhao Y, Yang J, et al. Cytosolic FoxO1 is essential for the induction of autophagy and tumour suppressor activity. Nat Cell Biol. 2010 Jul;12(7):665-75.

[5]Bhutani N, Piccirillo R, et al. Cathepsins L and Z are critical in degrading polyglutamine-containing proteins within lysosomes. J Biol Chem. 2012 May 18;287(21):17471-82.

[6]Katunuma N, Kominami E, et al. Structure, properties, mechanisms, and assays of cysteine protease inhibitors: cystatins and E-64 derivatives. Methods Enzymol. 1995;251:382-97.