PD-150606 (179528-45-1) is a selective, cell-permeable non-peptide calpain inhibitor (Ki for μ- and m-calpains = 0.21 and 0.37 μM respectively). Acts at the calcium binding site of calpain rather than the substrate-binding site. Inhibits calpain activity in two intact cell systems. Attenuates hypoxic/hypoglycemic injury to cerebrocortical neurons in culture and excitotoxic injury to Purkinje cells in cerebellar slices1. PD-150606 displays cytoprotective effects in oxidant- and calcium ionophore-induced cell death2. Some protective effects may be due to inhibition of MMP activity3.
1) Wang et al. (1996), An alpha-mercaptoacrylic acid derivative is a selective nonpeptide cell-permeable calpain inhibitor and is neuroprotective; Proc. Natl. Acad. Sci. USA, 93 6687
2) Waters et al. (1997), Calpains mediate calcium and chloride influx during the late phase of cell injury; J. Pharmacol. Exp. Therap., 283 1177
3) Ali et al. (2012), Calpain inhibitors exhibit matrix metalloproteinase-2 inhibitory activity; Biochem. Biophys. Res. Commun., 423 1