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Merck
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文件

330005

Sigma-Aldrich

EST

A cell-permeable, irreversible inhibitor of cysteine proteases.

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

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About This Item

经验公式（希尔记法）:
C17H30N2O5
CAS号:
88321-09-9
分子量:
342.43
MDL號碼:
MFCD00132883
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

化驗

≥97% (HPLC)

形狀

solid

製造商／商標名

Calbiochem®

儲存條件

OK to freeze

顏色

white

溶解度

DMSO: soluble

運輸包裝

ambient

儲存溫度

−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 密鑰

SRVFFFJZQVENJC-IHRRRGAJSA-N

一般說明

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)

重構

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

其他說明

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.

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 2

閃點（°F）

Not applicable

閃點（°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
Cong Zeng et al.
bioRxiv : the preprint server for biology (2021-06-09)
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is a highly transmissible coronavirus responsible for the global COVID-19 pandemic. Herein we provide evidence that SARS-CoV-2 spreads through cell-cell contact in cultures, mediated by the spike glycoprotein. SARS-CoV-2 spike is more efficient
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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
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