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Key Documents

330005

Sigma-Aldrich

EST

A cell-permeable, irreversible inhibitor of cysteine proteases.

Synonyme(s) :

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

Formule empirique (notation de Hill):
C17H30N2O5
Numéro CAS:
88321-09-9
Poids moléculaire :
342.43
Numéro MDL:
MFCD00132883
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥97% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze

Couleur

white

Solubilité

DMSO: soluble

Conditions d'expédition

ambient

Température de stockage

−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

Clé InChI

SRVFFFJZQVENJC-IHRRRGAJSA-N

Description générale

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.

Actions biochimiques/physiologiques

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

Avertissement

Toxicity: Irritant (B)

Reconstitution

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

Autres remarques

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.

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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