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E-64半胱氨酸蛋白酶(cysteine protease)抑制剂

E-64

产品编号:A2576
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) ¥550.00 现货
5mg ¥500.00 现货
25mg ¥1,400.00 现货
100mg ¥4,200.00 现货
250mg ¥9,800.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. Blass G, Levchenko V, et al. "Chronic cathepsin inhibition by E-64 in Dahl salt-sensitive rats." Physiol Rep. 2016 Sep;4(17). pii: e12950. PMID:27597769
2. Ying Long, Xuri Zhang, et al. "Initial events in the breakthrough of the epithelial barrier of the small intestine by Angiostrongylus cantonensis." Arch Biol Sci. 2016;68(2):375-383

该产品包含在以下化合物库中:

质量控制

化学结构

E-64

相关生物数据

E-64

相关生物数据

E-64

相关生物数据

E-64

相关生物数据

E-64

E-64 Dilution Calculator

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E-64 Molarity Calculator

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化学性质

CAS号 66701-25-5 SDF Download SDF
化学名 (2S,3S)-3-[[(2S)-1-[4-(diaminomethylideneamino)butylamino]-4-methyl-1-oxopentan-2-yl]carbamoyl]oxirane-2-carboxylic acid
SMILES CC(C)CC(C(=O)NCCCCN=C(N)N)NC(=O)C1C(O1)C(=O)O
分子式 C15H27N5O5 分子量 357.41
溶解度 ≥53.6mg/mL in DMSO 储存条件 Store at 2-8°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-64是一种天然的、有效的和不可逆的半胱氨酸蛋白酶抑制剂,作用于cathepsins K、S和L,IC50值分别为1.4、4.1和2.5 nM。.
靶点 cathepsins K cathepsins S cathepsins L      
IC50 1.4nM 4.1nM 2.5nM      

实验操作

细胞实验[1]:

细胞系

H-59和M-27细胞

溶解方法

在DMSO中的溶解度≥53.6mg/mL。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

10 μg/ml;48 h

应用

E-64以剂量依赖的方式抑制H-59细胞的侵袭,在10 μg/ml浓度时达到97%的最大抑制,是无毒性的。用包被7.5 μg/滤波器IV型胶原的过滤器测得细胞迁移仅减少25%,表明在缺乏基底膜屏障时,半胱氨酸蛋白酶在细胞迁移中发挥更加次要的作用。然而,E-64对M-27细胞的侵袭没有显著影响,甚至在高达100 μg/ml时。

动物实验[2]:

动物模型

Wistar系大鼠

剂量

1 mg/100 g体重;腹腔注射

应用

在注射E-64后1小时杀死动物,测定溶酶体中cathepsin B和cathepsin L的活性。结果表明,E-64抑制cathepsin B和cathepsin L的活性。

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] Navab R, Mort J S, Brodt P. Inhibition of carcinoma cell invasion and liver metastases formation by the cysteine proteinase inhibitor E-64. Clinical & experimental metastasis, 1997, 15(2): 121-129.

[2] Hashida S, TOWATARI T, KOMINAMI E, et al. Inhibitions by E-64 derivatives of rat liver cathepsin B and cathepsin L in vitro and in vivo. Journal of biochemistry, 1980, 88(6): 1805-1811.

View Related Products By Research Topics

研究更新

1. Conformational mobility of active and E-64-inhibited actinidin. Biochim Biophys Acta. 2013 Oct;1830(10):4790-9. doi: 10.1016/j.bbagen.2013.06.015. Epub 2013 Jun 23.
Abstract
Actinidin, a member of C1 family cysteine proteases, has many advantages, including a wide pH activity and wide substrate specificity, which make it a good model system to study enzyme-substrate interations.
2. In vitro ANTIGIARDIAL ACTIVITY OF THE CYSTEINE PROTEASE INHIBITOR E-64. Rev Inst Med Trop Sao Paulo. 2014 Jan-Feb;56(1):43-7. doi: 10.1590/S0036-46652014000100006.
Abstract
E-64, a cysteine protease inhibitor, decreased rates of Giardia trophozoites growth, adherence and viability by > 50% indicating it interferes in some crucial processes involved in parasite survival.
3. A Cathepsin B Inhibitor, E-64, Improves the Preimplantation Development of Bovine Somatic Cell Nuclear Transfer Embryos. J Reprod Dev. 2013 Nov 16. [Epub ahead of print]
Abstract
E-64 not only promoted blastocyst development of SCNT embryos but also increased the cryosurvival rates of IVF and SCNT blastocysts. IVF and SCNT blastocysts derived from E-64-treated group were characterized by increased total cell numbers, decreased apoptotic nuclei, suppressed Bax expression and stimulated Bcl-xL expression.
5. [Effect of different molarity cathepsins specific inhibitor E-64 on dentin-resin bonding durability]. Zhonghua Kou Qiang Yi Xue Za Zhi. 2013 Jun;48(6):368-71.
Abstract
E-64, a cathepsin inhibitor, has been investigated for its in vitro effect on dental endogenous cathepsins and its most effective molarity to elevate dentin-resin bouding durability.

产品描述

E-64(L-反式-环氧琥珀酰肽类化合物)是一种特异性的半胱氨酸蛋白酶抑制剂,从曲霉菌(Aspergillus)的培养物中分离获得。E-64可以抑制papain、ficin和bromelains[1]。

据报道,E-64可以抑制另外两种哺乳动物半胱氨酸蛋白酶:cathepsin L3和来自人乳腺癌组织的蛋白酶,也可以抑制来自鸡肌肉组织的钙依赖性蛋白酶calpain[5]。抑制数据的双倒数曲线显示,E-64与底物没有竞争性[1]。环氧琥珀酰部分的光学异构不会影响E-64对papain的抑制活性[6,7]。E-64最实际的应用是papain相关半胱氨酸蛋白酶的活性位点滴定(active-site titration),可用于确定酶浓度。

参考文献:
1.  A. J. BARRETT, A. A. KEMBHAVI, 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) 201, 189-198
2.  Hanada, K., Tamai, M., Yamagishi, M., Ohmura, S., Sawada, J. & Tanaka, I. (1978c) Agric. Biol. Chem. 42, 523-528
3.  Towatari, T., Tanaka, K., Yoshikawa, D. & Katunuma, N. (1978).J. Biochem. (Tokyo) 84, 659-671.
4.  Mort, J. S., Recklies, A. D. & Poole, A. R. (1980) Biochim. Biophys. Acta 614, 134-143.
5.  Sugita, H., Ishiura, S., Suzuki, K. & Imahori, K. (1980) J. Biochem. (Tokyo) 87, 339-341
6.  Hanada, K., Tamai, M., Morimoto, S., Adachi, T.,Ohmura, S., Sawada, J. & Tanaka, I. (1978a) Agric. Biol. Chem. 42, 537-541.
7.  Hanada, K., Tamai, M., Ohmura, S., Sawada, J., Seki, T.& Tanaka, I. (1978b)Agric. Biol. Chem. 42, 529-536
8.  Knight, C. G. (1980) Biochem. J. 189,447-453
9.  Takio, K., Towatari, T., Katunuma, N. & Titani, K.(1980) Biochem. Biophys. Res. Commun. 97, 340-346
10.  Bender, M. L., Begue-Canton, M. L., Blakeley, R. L.,Brubacher, L. J., Feder, J., Gunter, C. R., Kezdy, F. J.,Killheffer, J. V., Marshall, T. H., Miller, C. G., Roeske,R. W. & Stoops, J. K. (1966) J. Am. Chem. Soc. 88,5890-5913