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PotentinhibitoroftheH3K27histonedemethylasesJMJD3(KDM6B)andUTX(KDM6A)(IC50valuesare28and53nMrespectively).AlsoinhibitsKDM5B,KDM5CandKDM5A(IC50valuesare170,550and6,800nMrespectively).Exhibitsnoactivityagainstapanelofotherhistonedemethylases(IC50>20μM),anddisplaysnosignificantinhibitoryactivityagainst100proteinkinasesataconcentrationof30μM.Ethylesterderivativealsoavailable.
ThisprobeissuppliedinconjunctionwiththeStructuralGenomicsConsortium.Forfurthercharacterizationdetails,pleasevisittheGSKJ1probesummaryontheSGCwebsite.
GSKJ1isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight389.45.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Kruidenieretal(2012)AselectivejumonjiH3K27demethylaseinhibitormodulatestheproinflammatorymacrophageresponse.Nature488404PMID:22842901
Heinemannetal(2014)InhibitionofdemethylasesbyGSK-J1/J4.Nature514E1PMID:25279926
Keywords:GSKJ1,supplier,GSKJ1,histone,demethylases,inhibitors,inhibits,UTX,JMJD3,H3K27,epigenetics,jumonji,demethylation,sgc,Histone,Demethylases,Histone,Demethylases,TocrisBioscience
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