• 欢迎来到美国APExBIO中文站,专注小分子抑制剂、激动剂、拮抗剂及化合物库!

 


加 微 信 得 红 包
ApexBio
Search Site
相关产品
E 64d半胱氨酸蛋白酶抑制剂

E 64d

产品编号:A1903
ApexBio 的所有产品仅用作科研,我们不为任何个人用途提供产品和服务
规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥1,500.00 现货
1mg ¥500.00 现货
5mg ¥1,100.00 现货
25mg ¥4,200.00 现货
100mg ¥12,500.00 现货

电话: 021-55669583

Email: sales@apexbio.cn

全球经销商

Sample solution is provided at 25 µL, 10mM.

引用文献

1. Maxine Bauzon, Penelope M. Drake, et al. "Maytansine-bearing antibody-drug conjugates induce in vitro hallmarks of immunogenic cell death selectively in antigen-positive target cells." OncoImmunology.Received 09 Aug 2018, Accepted 12 Dec 2018, Published online: 22 Jan 2019.
2. An H, Harper JW. "Systematic analysis of ribophagy in human cells reveals bystander flux during selective autophagy." Nat Cell Biol. 2017 Dec 11. PMID:29230017
3. Tsai YC, Kotiya A, et al. "Deubiquitinating enzyme VCIP135 dictates the duration of botulinum neurotoxin type A intoxication." Proc Natl Acad Sci U S A. 2017 Jun 27;114(26):E5158-E5166. PMID:28584101

质量控制

化学结构

E 64d

相关生物数据

E 64d

相关生物数据

E 64d

相关生物数据

E 64d

相关生物数据

E 64d

相关生物数据

E 64d

E 64d Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

E 64d Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

化学性质

CAS号 88321-09-9 SDF Download SDF
化学名 ethyl (2S,3S)-3-[[(2S)-4-methyl-1-(3-methylbutylamino)-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylate
SMILES CCOC(=O)C1C(O1)C(=O)NC(CC(C)C)C(=O)NCCC(C)C
分子式 C17H30N2O5 分子量 342.43
溶解度 ≥17.1215mg/mL in DMSO 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

E-64d (合成的E-64的类似物、E-64c的乙基酯)是一个不可逆的、膜通透性的溶酶体和胞浆半胱氨酸蛋白酶抑制剂,抑制钙蛋白酶(calpain)和半胱氨酸蛋白酶cathepsins F、K、B、H和L。.
靶点 cathepsins F cathepsins K cathepsins B cathepsins H cathepsins L  
IC50            

实验操作

细胞实验[1]:

细胞系

血小板

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

50 μg/ml;10 min

应用

A23187和钙可以共同激活血小板,它们也可以导致calpain催化的ABP和talin蛋白水解。在缺乏抑制剂时,A23187导致ABP和talin的完全降解。E64d是细胞通透性的抑制剂,抑制细胞内的蛋白水解,有些抑制在最低测试浓度 20 μg/ml时观察到,而50μg/ml浓度的E 64d基本可以完全抑制蛋白水解。

动物实验[2]:

动物模型

雄性Sprague–Dawley大鼠

剂量

4 μg;腹腔注射

应用

E-64d治疗后,小鼠用penicillin处理诱导癫痫反复发作。结果表明,E-64d显著减少在齿状回颗粒上层和海马CA3区域的异常苔藓纤维发芽。在无E-64d治疗大鼠中,在齿状回和CA3区域的锥体层有明显的苔藓纤维末端聚集。而在E-64d治疗大鼠中,在齿状回颗粒上层和CA3区域中的苔藓纤维末端聚集显著减少。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] McGowan E B, Becker E, Detwiler T C. Inhibition of calpain in intact platelets by the thiol protease inhibitor E-64d. Biochemical and biophysical research communications, 1989, 158(2): 432-435.

[2] Ni H, Ren S, Zhang L, et al. Expression profiles of hippocampal regenerative sprouting-related genes and their regulation by E-64d in a developmental rat model of penicillin-induced recurrent epilepticus. Toxicology letters, 2013, 217(2): 162-169.

View Related Products By Research Topics

研究更新

1. Expression profiles of hippocampal regenerative sprouting-related genes and their regulation by E-64d in a developmental rat model of penicillin-induced recurrent epilepticus. Toxicol Lett. 2013 Feb 27;217(2):162-9. doi: 10.1016/j.toxlet.2012.12.010. Epub 2012 Dec 21.
Abstract
E-64d inhibited hippocampal aberrant mossy fiber sprouting and seizure-induced up-regulation of ApoE and Clusterin in rats. A significant down-regulation of PRG-1, PRG-3, prg-5, cathepsin B amd ApoE and a up-regulation of nSMase and ANX7 were observed in hippocampus of E-64d-pretreated seizure rats.
2. Detecting autophagy in Arabidopsis roots by membrane-permeable cysteine protease inhibitor E-64d and endocytosis tracer FM4-64. Plant Signal Behav. 2011 Dec;6(12):1946-9.
Abstract
In order to detect autophage, E-64d, a membrane-permeable cysteine protease inhibitor, was applied in culture medium where root tips from Arabidopsis seedlings were incubated.
3. [Inhibition of calpain expression by E-64d in the rat retina subjected to ischemia/reperfusion injury]. Mol Biol (Mosk). 2008 Mar-Apr;42(2):258-64.
Abstract
E-64d exhibits protective effects against IRI-induced retinal apoptosis, since it inhibited IRI-induced up-regulation of m-calpain expression, the crease of m-calpain/calpastatin ratio and IRI-induced retinal damage in rats.
4. Inhibition of calpain in intact platelets by the thiol protease inhibitor E-64d. Biochem Biophys Res Commun. 1989 Jan 31;158(2):432-5.
Abstract
E-64d is a membrane permeant inhibitor of calpain that enters intact cells and inhibits proteolysis once it’s incubated with platelets before lysis.
5. CB-64D and CB-184: ligands with high sigma 2 receptor affinity and subtype selectivity. Eur J Pharmacol. 1995 May 24;278(3):257-60.
Abstract
CD-64L, CB-64D, CB-182 and CB-184 exhibited sigma 1 and sigma 2 Ki of 10.5 and 154 nM, 3063 and 16.5 nM, 27.3 and35.5 nM and 7436 and 13.4 nM respectively, where CB-64D and CB-184 displayed high sigma 2 receptor affinity and subtype selectivity.

产品描述

E-64d是E-64c的膜通透性衍生物和巯基蛋白酶的抑制剂,被用于检测其对完整血小板中钙蛋白酶(calpain)的抑制活性。

E-64c或E-64d均可以抑制钙蛋白酶的活性。将完整血小板与抑制剂孵育10分钟,在裂解前洗去细胞外的抑制剂,E-64c和leupeptin均不能抑制蛋白水解,但E-64d可以。E-64d能够进入血小板,不会通过洗涤而除去。然而,E-64c和E-64d均能够抑制裂解血小板中的蛋白酶活性。由于该蛋白酶的活性是Ca2+依赖型的,而且能够被钙蛋白酶抑制剂抑制,因而被认为是钙蛋白酶。E-64d能够进入完整的血小板:i)洗涤除去细胞外的抑制剂,裂解血小板后检测不到蛋白酶活性;ii)与E-64d而非E-64c孵育,可以激活血小板,从而抑制由A23187和钙激活的完整血小板中钙蛋白酶的水解活性。

参考文献:
1.  M. Tamai, K. Matsumoto, S. Omura, I. Koyama, Y. Ozawa, K. Hanada J. Pharmacobio-Dyn., 9 (1986), pp. 672–677.
2.  E. B. McGowan, E. Becker, and T. C. Detwiler, INHIBITION OF CALPAIN IN INTACT PLATELETS BY THE THIOL PROTEASE INHIBITOR E-64d. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS , Vol. 158, No. 2, 1989.
3.  Carmen JC, Sinai AP. The Differential Effect of Toxoplasma Gondii Infection on the Stability of BCL2-Family Members Involves Multiple Activities. Front Microbiol. 2011 Jan 24; 2:1.