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PanJumonjihistonedemethylaseinhibitor(IC50valuesare230,340,435,445,855and1100nMforJARID1A,JMJD2E,JMJD2B,JMJD2A,JMJD3andJMJD2Crespectively).ExhibitsnegligIBLeactivityatPHD2andTET1.SelectivelyblockscancercellgrowthinvitroanddiminishestumorgrowthinH358andA549mousexenograftmodelsinvivo.Prolongssurvivalinamousemodelofbreastcancer.
JIB04isalsoofferedaspartoftheTocriscreenPlusandTocriscreenEpigeneticsToolbox.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Thefollowingdataisbasedontheproductmolecularweight308.76.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Referencesarepublicationsthatsupporttheproducts'biologicalactivity.
Wangetal(2013)AsmallmoleculemodulatesJumonjihistonedemethylaseactivityandselectivelyinhibitscancergrowth.Nat.Commun.42035PMID:23792809
GrunickeandHofmann(1997)AzinylanddiazinylhydrazonesderivedfromarylN-heteroarylketones:synthesisandantiproliferativeactivity.J.Med.Chem.404420PMID:9435912
Keywords:JIB04,supplier,JIB04,histone,demethylases,inhibits,inhibitors,JMJ,JARID1A,JMJD2A,JMJD2B,JMJD2C,JMJD2E,JMJD3,pan,selective,antiproliferative,Histone,Demethylases,Histone,Demethylases,TocrisBioscience
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