Biochem/physiol Actions

Reversible: no

Product does not compete with ATP.

Primary Targetcalpain-1

Cell permeable: yes

Target IC₅₀: 10-100 µM for calpain-1

General description

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.

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.

Legal Information

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

Other Notes

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.

Packaging

1 mg in Plastic ampoule

Reconstitution

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

Warning

Toxicity: Irritant (B)