PD150606

PD150606 is a selective, cell-permeable, non-peptide small molecule inhibitor of calpain, specifically targeting both μ-calpain (calpain-1) and m-calpain (calpain-2) with Ki values of approximately 0.21 μM and 0.37 μM respectively[1][3][5]. It acts noncompetitively at the calcium-binding site of calpains rather than the substrate-binding site[3][9]. PD150606 exhibits high specificity for calpains over other proteases such as cathepsin B and L[3]. Mechanistically, it inhibits calpain-mediated processes including apoptosis by preventing the cleavage and nuclear translocation of apoptosis-inducing factor (AIF), thereby showing neuroprotective effects in various neuronal injury models such as glutamate-induced spiral ganglion neuron apoptosis and hypoxic/hypoglycemic injury to neurons[4][7][9]. It has also demonstrated cytoprotective effects in models of ischemia/reperfusion injury[10] and can reduce excitotoxicity-dependent motor neuron death[8]. PD150606 is used exclusively for research purposes; it is not approved for clinical use in humans.

Other names

3-(4-iodophenyl)-2-mercapto-(Z)-2-propenoic acid(Z)-3-(4-iodophenyl)-2-sulfanylprop-2-enoic acid