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PotentandselectiveBRD4bromodomaininhibitor(Ki=30-50nMforthefirstbromodomain(BRD4(1)).Exhibits10-foldselectivityforBRD4(1)overBRD4(2).BlocksBRD4transcriptionalactivityinlipopolysaccharide-inducedproductionofbothnitricoxideandIL-6inmousemacrophages(IC50valuesare3.8and4.9μM,respectively).Attenuatesmelanomacellproliferationinvitro.
SoldunderlicensefromIcahnSchoolofMedicineatMountSinai.
MS436isalsoofferedaspartoftheTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight383.42.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Zhangetal(2013)Structure-guideddesignofpotentdiazobenzeneinhibitorsfortheBETbromodomains.J.Med.Chem.569251PMID:24144283
Seguraetal(2013)BRD4sustainsmelanomaproliferationandrepresentsanewtargetforepigenetictherapy.CancerRes.736264PMID:23950209
Keywords:MS436,supplier,MS436,potent,selective,BRD4,BrD1,Bromodomain,inhibitors,inhibits,BrD2,gene,transcription,transcriptional,epigenetics,BRD4(1),Bromodomains,Bromodomains,TocrisBioscience
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