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PotentandselectiveallostericinhibitorofWip1phosphatase(IC50=6nM).ExhibitsselectivityforWip1over21otherphosphatases.IncreasesphosphorylationofWip1substrates,includingp53,Chk2,H2AXandATM.Attenuatestumorcellgrowthinavarietyoflymphoidcelllines.Alsoinhibitslymphomaxenograftgrowthinvivo.Orallybioavailable.
SoldforresearchpurposesonlyunderagreementfromGlaxoSmithKline
GSK2830371isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight461.02.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Gilmartinetal(2014)AllostericWip1phosphataseinhibitionthroughflap-suBDomaininteraction.Nat.Chem.Biol.10181PMID:24390428
Keywords:GSK2830371,supplier,GSK2830371,potent,selective,allosteric,inhibitors,inhibits,wip1,phosphatases,antitumor,orally,bioavailable,Protein,Ser/Thr,Phosphatases,Protein,Ser/Thr,Phosphatases,TocrisBioscience
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