OTS193320-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOTS193320Cat.No.:HY-122182CASNo.:2093401-33-1分?式:C??H??ClN?O?分?量:536.02作?靶點(diǎn):HistoneMethyltransferase;Apoptosis作?通路:Epigenetics;Apoptosis儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性O(shè)TS193320?種咪唑并[1,2-a]吡啶化合物，?種SUV39H2甲轉(zhuǎn)移酶活性抑制劑。OTS193320降低乳腺癌細(xì)胞中的全局組蛋?H3賴氨酸9三甲化?平并引發(fā)凋亡細(xì)胞死亡。與單?藥劑OTS193320或DOX相?，OTS193320與Doxorubicin(DOX;HY-15142A)的組合可以導(dǎo)致γ-H2AX?平以及癌細(xì)胞活?的降低。IC50&TargetSUV39H2/KMT1B體外研究OTS193320(0.125-0.5μM;24hours)hasgrowthinhibitoryeffectonbreastcancercelllines.OTS193320exhibitsahighinhibitoryeffectagainstSUV39H2enzymaticactivity(IC50=22.2nM)andagrowthsuppressiveeffectofSUV39H2-positiveA549lungcancercells(IC50=0.38μM)[1].OTS193320(0.5μM;48hours)inducesapoptosisinbreastcancercells[1].OTS193320(0.125-0.5μM;24hours)causesattenuationofH3K9me3levelsinadose-dependentmanner[1].OTS193320sensitizesbreastcancercellstodoxorubicinviaattenuationofγ-H2AX.CombinationofOTS193320anddoxorubicin(DOX)significantlyattenuatescancercellviabilityinvitro,comparedtosingleagenttreatmentofeitherdrug[1].CellViabilityAssay[1]CellLine:MCF-7,SK-BR-3,ZR-75-1,T-47D,MDA-MB-231,BT-20breastcancercelllinesConcentration:0-1μMIncubationTime:72hours1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:HadGrowthinhibitoryeffectonMCF-7,SK-BR-3,ZR-75-1,T-47D,MDA-MB-231,andBT-20breastcancercelllineswithIC50valuesfrom0.41to0.56μM,respectively.ApoptosisAnalysis[1]CellLine:MDA-MB-231andBT-20cellsConcentration:0.5μMIncubationTime:48hoursResult:Showedanincreaseinthenumberofcellsatearly-andlate-stageapoptosis.WesternBlotAnalysis[1]CellLine:MDA-MB-231andBT-20cellsConcentration:0.125,0.25,0.5μMIncubationTime:24hoursResult:CausedattenuationofH3K9me3levelsinadose-dependentmanner.REFERENCES[1].TheodoreVougiouklakis,etal.DevelopmentofnovelSUV39H2inhibitorsthatexhibitgrowthsuppressiveeffectsinmousexenograftmodelsandregulatethephosphorylationofH2AX.Oncotarget.2018Aug7;9(61):31820-31831.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu