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PotentandselectiveATP-competitiveDyrk1Bkinaseinhibitor(IC50=7nM);displaysdistinctcellulareffectswhencomparedtoDYRK1BknockdownthroughsiRNA.Demonstratescellularinvitroactivity(IC50=194nM).ExhibitsbetterselectivitythanAZ191(Cat.No5232);displaysnooff-targeteffectsagainstapanelof124kinasestested(nokinasewasinhibitedabove50%at1μM).
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight300.36.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Kettleetal(2015)DiscoveryandoptimizationofanovelseriesofDyrk1BkinaseinhibitorstoexploreaMEKresistancehypothesis.J.Med.Chem.582834PMID:25738750
Keywords:AZDyrk1B33,supplier,AZDyrk1B33,Dyrk1B,kinase,inhibitors,inhibits,dual,specificity,tyrosine,phosphorylation,regulated,kinases,potent,DYRK,DYRK,TocrisBioscience
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