Biochem/physiol Actions

Target K_i: 210 nM for calpain-1 and 370 nM for calpain-2

Primary TargetCalpain-1

Reversible: no

Product does not compete with ATP.

Cell permeable: yes

General description

A cell-permeable, selective non-peptide calpain inhibitor (K_i = 210 nM for calpain I and 370 nM for calpain II) directed towards the calcium- binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and L. PD 150606 is a non-competitive inhibitor with respect to the substrate and does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis of thymocytes.

A cell-permeable, non-competitive, selective non-peptide calpain inhibitor [K_i = 210 nM for calpain-1 (Cat. Nos. 208712 and 208713) and 370 nM for calpain-2 (Cat. Nos. 208715 and 208718)] directed towards the calcium binding sites of calpain. Exhibits high specificity for calpains relative to other proteases, such as cathepsin B and cathepsin L. Does not shield calpain against inactivation by the active-site inhibitor trans-(epoxysuccinyl)-L-leucyl-amido-3-methylbutane. Reportedly prevents dexamethasone-induced apoptosis in thymocytes.

Legal Information

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

Other Notes

Lin, G.D., et al. 1997. Nat. Struct. Biol. 4, 539.Squier, M.K., and Cohen, J.J. 1997. J. Immunol. 158, 3960.Edelstein, C.L., et al. 1996. Kidney Int. 50, 1150.Wang, K.K.W., et al. 1996. Proc. Natl. Acad. Sci. USA 93, 6687.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

Warning

Toxicity: Standard Handling (A)