Overview | Acell-permeable,pyrazoloneGSK-3βinhibitor(IC50=34nM,inanenzymaticassay)thatishighlyselectiveamongapanelof40kinasesthathavebeenprofiledwithmorethan50foldselectivity.Itexhibitsnooff-targetactivityagainstapanelof44humanandrodentCNSreceptors,channels,andtransportersexceptforsomemodestactivitytoward5HT1a.Itdemonstratesneuroprotectiveactivityofneuronsinanoxidativestressmodelinducedbyhomocysteicacid(HCA)from1–20μM,withoutobservablecytotoxicity,andissuperiortoSB-216763Cat.No.361566)at5μMincellmicrographs.Inaddition,itisshowntoattenuatelocomotoractivityinanchlordiazepoxide/amphetamine-inducedhyperactivitymicemodelinvivoat150mg/kg. |