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Merck
CN
所有图片(1)

文件

330005

Sigma-Aldrich

EST

A cell-permeable, irreversible inhibitor of cysteine proteases.

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别名:
EST, Loxistatin, (2S,3S)- trans-Epoxysuccinyl-L-leucylamido-3-methylbutane Ethyl Ester, E-64d, Loxistatin, (2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane Ethyl Ester, E-64d
经验公式(希尔记法):
C17H30N2O5
CAS号:
分子量:
342.43
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

检测方案

≥97% (HPLC)

形式

solid

制造商/商品名称

Calbiochem®

储存条件

OK to freeze

颜色

white

溶解性

DMSO: soluble

运输

ambient

储存温度

−20°C

InChI

1S/C17H30N2O5/c1-6-23-17(22)14-13(24-14)16(21)19-12(9-11(4)5)15(20)18-8-7-10(2)3/h10-14H,6-9H2,1-5H3,(H,18,20)(H,19,21)/t12-,13-,14-/m0/s1

InChI key

SRVFFFJZQVENJC-IHRRRGAJSA-N

一般描述

A cell-permeable, irreversible inhibitor of cysteine proteases. Similar to E-64 (Cat. No. 324890) but devoid of charged groups. Reported to inhibit calpain-1 activation. The inhibitory activity of EST has been attributed to E-64c, the free acid formed by hydrolysis of the ester in vivo. Used in animal models of muscular dystrophy.
A cell-permeable, irreversible inhibitor of cysteine proteases. Similar to E-64 (Cat. No. 324890) but is devoid of charged groups. The inhibitory activity of EST has been attributed to E-64c, the free acid formed by hydrolysis of the ester in vivo. Used in animal models of muscular dystrophy. Recommended working concentration is 10-100 µM.

生化/生理作用

Cell permeable: yes
Primary Target
calpain-1
Product does not compete with ATP.
Reversible: no
Target IC50: 10-100 µM for calpain-1

警告

Toxicity: Irritant (B)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for 6 months at -20°C.

其他说明

Inomata, M., et al. 1996. Arch. Biochem. Biophys. 328, 129.
Mehdi, S. 1991. Trends Biochem. Sci. 16, 150.
McGowan, E.B., et al. 1989. Biochem. Biophys. Res. Commun.158, 432.
Tamai, M., et al. 1987. J. Pharmacobiodyn.10, 678.
Komatsu, K., et al. 1986. Exp. Neurol. 91, 23.
Tamai, M., et al. 1986. J. Pharmacobiodyn. 9, 672.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Zhifen Cui et al.
Nature chemical biology, 18(10), 1056-1064 (2022-07-26)
SARS-CoV-2 entry into cells requires specific host proteases; however, no successful in vivo applications of host protease inhibitors have yet been reported for treatment of SARS-CoV-2 pathogenesis. Here we describe a chemically engineered nanosystem encapsulating CRISPR-Cas13d, developed to specifically target
S Birken et al.
The Journal of endocrinology, 171(1), 131-141 (2001-09-27)
The gonadotropins are a family of closely related heterodimeric glycoprotein hormones homologous in structure to disulfide-knot growth factors. Metabolic proteolytic processing in vivo of this disulfide cross-linked region results in urinary excretion of a residual highly stable core structure. The
Naoko Iwata-Yoshikawa et al.
Nature communications, 13(1), 6100-6100 (2022-10-16)
In cultured cells, SARS-CoV-2 infects cells via multiple pathways using different host proteases. Recent studies have shown that the furin and TMPRSS2 (furin/TMPRSS2)-dependent pathway plays a minor role in infection of the Omicron variant. Here, we confirm that Omicron uses
Panke Qu et al.
mBio, 14(1), e0317622-e0317622 (2023-01-11)
The rapid spread and strong immune evasion of the SARS-CoV-2 Omicron subvariants has raised serious concerns for the global COVID-19 pandemic. These new variants exhibit generally reduced fusogenicity and increased endosomal entry pathway utilization compared to the ancestral D614G variant
Inmaculada Serramito-Gómez et al.
Autophagy, 18(12), 3023-3030 (2022-03-22)
A coding allele of ATG16L1 that increases the risk of Crohn disease (T300A; rs2241880) impairs the interaction between the C-terminal WD40 domain (WDD) and proteins containing a WDD-binding motif, thus specifically inhibiting the unconventional autophagic activities of ATG16L1. In a

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