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PotentandselectivePERKinhibitor(IC50=6nM).Exhibits>160-foldselectivityforPERKoverB-RafandGCN2,aswellasapanelof387otherkinases.Orallybioavailable.
Bypermissionoftheauthors
AMGPERK44isalsoofferedaspartoftheTocriscreenPlusandTocriscreenKinaseInhibitorToolboxII.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight561.07.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Smithetal(2015)Discoveryof1H-pyrazol-3(2H)-onesaspotentandselectiveinhibitorsofproteinkinaseR-likeendoplasmicreticulumkinase(PERK).J.Med.Chem.581426PMID:25587754
Keywords:AMGPERK44,supplier,AMGPERK44,PERK,inhibitors,inhibits,potent,selective,protein,kinase,R-like,PKR,ER,orally,bioavailable,PERK,PERK,TocrisBioscience
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