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. Displays cytoprotective effects in oxidant- and calcium ionophore-induced cell death2. Some protective effects may be due to inhibition of MMP activity3.
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