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PotentBETbromodomaininhibitor;exhibitsinhibitoryactivityatbromodomain-containingprotein(BRD)2andBRD4(IC50valuesare98and220nMrespectively).InducesapoptosisandG1cellcyclearrestinBETinhibitor-sensitivecelllines(MV4;11).AlsodownregulatesAuroraBexpressioninMV4;11cells.Cellpermeable.
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisitthePFI1probesummaryontheSGCwebsite.
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofPFI1isreviewedonthechemicalprobeswebsite.
PFI1isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight347.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Fishetal(2012)Identificationofachemicalprobeforbromoandextrac-terminalbromodomaininhibitionthroughoptimizationofafragment-derivedhit.J.Med.Chem.[Epubaheadofprint]PMID:23095041
Picaudetal(2013)PFI-1-ahighlyselectiveproteininteractioninhibitortargetingBETbromodomains.CancerRes.[Epubaheadofprint]PMID:
Keywords:PFI1,supplier,PFI1,bet,bromodomain,brd4,brd2,inhibitors,inhibits,epigenetics,atypical,kinases,bromodomain-containing,2,bromodomain-containing,4,sgc,Bromodomains,Bromodomains,TocrisBioscience
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