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蛋白酶抑制剂E 64 /E-64 {[allProObj[0].p_purity_real_show]}

货号:A252147 同义名: Proteinase inhibitor E 64 Ambeed 开学季,买赠积分,赢豪礼

E-64(蛋白酶抑制剂E 64)是一种高效的不可逆广谱半胱氨酸蛋白酶抑制剂,对木瓜蛋白酶的IC50为9 nM。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
E-64 化学结构 CAS号:66701-25-5
E-64 化学结构
CAS号:66701-25-5
E-64 3D分子结构
CAS号:66701-25-5
E-64 化学结构 CAS号:66701-25-5
E-64 3D分子结构 CAS号:66701-25-5
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E-64 纯度/质量文件 产品仅供科研

货号:A252147 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Cysteine Protease 其他靶点 纯度
Z-FA-FMK {[allProObj[0].p_purity_real_show]}
Leupeptin hemisulfate {[allProObj[0].p_purity_real_show]}
PMSF {[allProObj[0].p_purity_real_show]}
PD 151746 +

μ-Calpain, IC50: 260 nM

m-calpain, IC50: 5.33 μM

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Odanacatib ++++

Cathepsin K (human), IC50: 0.2 nM

Cathepsin K (rabbit), IC50: 1 nM

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E-64 +++

Cysteine protease, IC50: 9 nM

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E 64c {[allProObj[0].p_purity_real_show]}
E-64d {[allProObj[0].p_purity_real_show]}
MG-101 {[allProObj[0].p_purity_real_show]}
Calpeptin ++

Calpain II (porcine kidney), ID50: 40 nM

Calpain I (porcine erythrocytes), ID50: 52 nM

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Cathepsin inhibitor 1 +++

Cathepsin L, pIC50: 7.9

Cathepsin L2, pIC50: 5.5

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

E-64 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]

E-64 动物研究

Dose Mice: 1 mg/kg[7] (i.p.)
Administration i.p.

E-64 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.

E-64 实验方案

计算器
存储液制备 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

E-64 技术信息

CAS号66701-25-5
分子式C15H27N5O5
分子量 357.405
别名 Proteinase inhibitor E 64
运输蓝冰
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
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