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BETbromodomaininhibitor;blocksrecruitmentofBETtochromatin.InducesapoptosisandG0/G1cellcyclearrestinMLL-fusionleukemiccelllinesinvitro(IC50valuesare15,26,120and192nMforNOMO1,MV4;11,MOLM13andRS4;11celllinesrespectively);reducesBCL2expressioninNOMO1cells.ImprovessurvivalintworodentmodelsofMLL-fusionleukemiainvivo.EnhancesdifferentiationofhumaniPSCintomegakaryocytes.
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
Chemicalprobes.orgisaportalthatoffersindependentguidanceontheselectionand/orapplicationofsmallmoleculesforresearch.TheuseofI-BET151isreviewedonthechemicalprobeswebsite.
I-BET151dihydrochlorideisalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight488.37.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Dawsonetal(2011)InhibitionofBETrecruitmenttochromatinasaneffectivetreatmentforMLL-fusionleukaemia.Nature478529PMID:21964340
Fengetal(2014)Scalablegenerationofuniversalplateletsfromhumaninducedpluripotentstemcells.StemCellReports3817PMID:25418726
Keywords:I-BET151dihydrochloride,supplier,I-BET151,epigenetics,bet,bromodomains,inhibits,inhibitors,chromatin,recruitment,readers,antileukemia,MLL,fusion,induces,apoptosis,Bromodomains,ESCs,and,iPSC,Bromodomains,TocrisBioscience
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