Description
AR-A014418isaninhibitorofGSK-3βthatexhibitsanticancer,analgesic,cognitionenhancing,neuroprotective,andanti-inflammatoryactivities.AR-A014418decreasescellviABIlityanddownregulatesexpressionofsplicingfactors,Bcl-2,Bcl-xl,survivin,andMCL-1ingliomacells.Inmodelsofneuropathicpain,AR-A014418inhibitsthermalhyperalgesiaandmechanicalallodynia,potentiallythroughsuppressingexpressionofglutamatetransporterGLT-1.Thiscompoundalsoinhibitsthedevelopmentoflearningandmemorydeficitsinanimalmodelsofdiabetes.Inspinalcordinjurymodels,AR-A014418preventsmitochondrialapoptosisanddecreaseslevelsofpro-inflammatorycytokines.
References
YadavAK,VashishtaV,JoshiN,etal.AR-A014418UsedagainstGSK3betaDownregulatesExpressionofhnRNPA1andSF2/ASFSplicingFactors.JOncol.2014;2014:695325.PMID:24550987.
WengHR,GaoM,MaixnerDW.Glycogensynthasekinase3betaregulatesglialglutamatetransporterproteinexpressioninthespinaldorsalhorninratswithneuropathicpain.ExpNeurol.2014Feb;252:18-27.PMID:24275526.
KingMR,AndersonNJ,GuernseyLS,etal.Glycogensynthasekinase-3inhibitionpreventslearningdeficitsindiabeticmice.JNeurosciRes.2013Apr;91(4):506-14.PMID:23362012.
TunçdemirM,YıldırımA,KaraoğlanA,etal.AR-A014418asaglycogensynthasekinase-3inhibitor:anti-apoptoticandtherapeuticpotentialinexperimentalspinalcordinjury.Neurocirugia(Astur).2013Jan-Feb;24(1):22-32.PMID:23116585.
