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Merck
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Documentos clave

330005

Sigma-Aldrich

EST

A cell-permeable, irreversible inhibitor of cysteine proteases.

Sinónimos:

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

Fórmula empírica (notación de Hill):
C17H30N2O5
Número de CAS:
88321-09-9
Peso molecular:
342.43
Número MDL:
MFCD00132883
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

100

descripción

RTECS - RR0404300

Ensayo

≥97% (HPLC)

Formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze

color

white

solubilidad

DMSO: soluble

Condiciones de envío

ambient

temp. de almacenamiento

−20°C

cadena SMILES

N([C@@H](CC(C)C)C(=O)NCCC(C)C)C(=O)[C@H]1O[C@@H]1C(=O)OCC

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

Clave InChI

SRVFFFJZQVENJC-IHRRRGAJSA-N

Descripción general

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.

Acciones bioquímicas o fisiológicas

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

Advertencia

Toxicity: Irritant (B)

Reconstitución

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

Otras notas

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.

Información legal

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

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 2

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable

Certificados de análisis (COA)

Busque Certificados de análisis (COA) introduciendo el número de lote del producto. Los números de lote se encuentran en la etiqueta del producto después de las palabras «Lot» o «Batch»

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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
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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
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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
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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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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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