PU139-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPU139Cat.No.:HY-124696CASNo.:158093-65-3分⼦式:C₁₂H₇FN₂OS分⼦量:246.26作⽤靶点:HistoneAcetyltransferase作⽤通路:Epigenetics储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:12.5mg/mL(50.76mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.0607mL20.3037mL40.6075mL5mM0.8121mL4.0607mL8.1215mL10mM0.4061mL2.0304mL4.0607mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性PU139⼀种有效的泛组蛋⽩⼄酰转移酶(HAT)抑制剂。PU139阻断HATsGcn5、p300/CBP相关因⼦(PCAF)、CBP和p300，IC50分别为8.39、9.74、2.49和5.35μM。IC50&TargetGCN5CBPp300PCAF8.39μM(IC50)2.49μM(IC50)5.35μM(IC50)9.74μM(IC50)体外研究PU139inhibitscellgrowthwithGI50sof[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEPU139(0-100μM;24-72hours)triggerscaspase-independentcelldeathintheneuroblastomacelllineSK-N-SH[1].体内研究PU139(25mg/kg;i.p.)synergizeswithDoxorubicinusedasaprototypicchemotherapeuticdrugingrowthinhibition[1].AnimalModel:MaleNMRI:nu/numice(Neuroblastomaxenografts)[1]Dosage:25mg/kgAdministration:Intraperitoneally(PU139)withDxorubicinat8ꢀmg/kgi.v.;Administeredondays14and21asasingledoseofeachcompoundor,forcombinationtherapy;bothdrugswereadministeredsuccessivelywithin1ꢀh.Result:OptimumgrowthinhibitionfollowingasinglePU139therapywasmoderate,butsignificantascomparedwiththeuntreatedgroupandconfirmedthepreviousfindings.REFERENCES[1].GajerJM,etal.Histoneacetyltransferaseinhibitorsblockneuroblastomacellgrowthinvivo.Oncogenesis.2015;4(2):e137.Published2015Feb9.[2].CarneiroVC,etal.Epigeneticchangesmodulateschistosomeeggformationandareanoveltargetforreducingtransmissionofschistosomiasis.PLoSPathog.2014;10(5):e1004116.Published2014May8.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly