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PotentandselectiveBRD1andTAF1inhibitor(IC50valuesare6-67and8-13nM,respectively).Displaysselectivityoverotherbromodomains(>30-foldoverothermembersoftheBRPFfamily;BRD9andATAD2;>300-foldoverBRD4).DisplaysBRD1andTAF1inhibitioninaNanoBRETcellassay.InhibitsbindingofBRD1andTAF1tohistoneH4(IC50valuesare575nMand0.9μM,respectively)andhistoneH3.3(IC50valuesare825nMand1.4μM,respectively).
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheBAY299probesummaryontheSGCwebsite.
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofBAY299isreviewedontheChemicalProbeswebsite.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight429.47.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Kleinetal(2014)CrosstalkbetweenepigeneticreadersregulatestheMOZ/MORFHATcomplexes.Epigenetics9186PMID:24169304
Boucheetal(2017)BenzoisoquinolinedionesaspotentandselectiveinhibitorsofBRPF2andTAF1/TAF1Lbromodomains.J.Med.Chem.604002PMID:28402630
Keywords:BAY299,supplier,BAY299,potent,BRD1,TAF1,inhibitors,inhibits,bromodomains,and,PHD,Finger,Transcription,initiation,factor,TFIID,subunits,1,Bromodomains,Bromodomains,TocrisBioscience
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