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Highaffinityandselectivecell-permeablep300/CBP-associatedfactor(PCAF)inhibitor(Ki=47nM).Exhibitsnosignificantactivityagainstapanelof48otherbromodomainsexceptGCN5(Kd=600nM).Exhibits>4500-foldselectivityforPCAFoverBRD4.AlsoexhibitsmetabolicstABIlityinmouseandhumanlivermicrosomesandnoobservablecytotoxicityinperipheralbloodmononuclearcells(PBMC).
ThiscompoundissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheL-MosesprobesummaryontheSGCwebsite.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight433.38.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Moustakimetal(2017)DiscoveryofaPCAFbromodomainchemicalprobe.Angew.Chem.Int.Ed.56827PMID:27966810
Keywords:LMosesdihydrochloride,supplier,PCAF,p300/CBP-associated,factor,GCN5,general,control,non-derepressIBLe,5,inhibitors,inhibits,high,affinity,selective,cell-permeable,2079885-05-3,Bromodomains,Bromodomains,TocrisBioscience
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