PD 150606

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.

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.

Cell permeable: yes

Primary Target
Calpain-1

Product does not compete with ATP.

Reversible: no

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

Packaged under inert gas

Toxicity: Standard Handling (A)

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

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.

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