GSK-3beta Inhibitor XXVI - Calbiochem

This product has been discontinued.

A cell-permeable, pyrazolone GSK-3β inhibitor (IC₅₀ = 34 nM, in an enzymatic assay) that is highly selective among a panel of 40 kinases that have been profiled with more than 50 fold selectivity. It exhibits no off-target activity against a panel of 44 human and rodent CNS receptors, channels, and transporters except for some modest activity toward 5HT1a. It demonstrates neuroprotective activity of neurons in an oxidative stress model induced by homocysteic acid (HCA) from 1–20 µM, without observable cytotoxicity, and is superior to SB-216763 Cat. No. 361566) at 5 µM in cell micrographs. In addition, it is shown to attenuate locomotor activity in an chlordiazepoxide/amphetamine-induced hyperactivity mice model in vivo at 150 mg/kg.