PU139-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPU139Cat.No.:HY-124696CASNo.:158093-65-3分?式:C??H?FN?OS分?量:246.26作?靶點:HistoneAcetyltransferase作?通路:Epigenetics儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(50.76mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.0607mL20.3037mL40.6075mL5mM0.8121mL4.0607mL8.1215mL10mM0.4061mL2.0304mL4.0607mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性PU139?種有效的泛組蛋??酰轉(zhuǎn)移酶(HAT)抑制劑。PU139阻斷HATsGcn5、p300/CBP相關(guān)因?(PCAF)、CBP和p300，IC50分別為8.39、9.74、2.49和5.35μM。IC50&TargetGCN5CBPp300PCAF8.39μM(IC50)2.49μM(IC50)5.35μM(IC50)9.74μM(IC50)體外研究PU139inhibitscellgrowthwithGI50sof[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEPU139(0-100μM;24-72hours)triggerscaspase-independentcelldeathintheneuroblastomacelllineSK-N-SH[1].體內(nèi)研究PU139(25mg/kg;i.p.)synergizeswithDoxorubicinusedasaprototypicchemotherapeuticdrugingrowthinhibition[1].AnimalModel:MaleNMRI:nu/numice(Neuroblastomaxenografts)[1]Dosage:25mg/kgAdministration:Intraperitoneally(PU139)withDxorubicinat8?mg/kgi.v.;Administeredondays14and21asasingledoseofeachcompoundor,forcombinationtherapy;bothdrugswereadministeredsuccessivelywithin1?h.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