STAT3-IN-10-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESTAT3-IN-10Cat.No.:HY-146728CASNo.:2499491-04-0分⼦式:C₁₇H₁₃NO₅分⼦量:311.29作⽤靶点:STAT;Apoptosis作⽤通路:JAK/STATSignaling;StemCell/Wnt;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性STAT3-IN-10⼀种STAT3抑制剂，IC50为5.18µM。STAT3-IN-10与STAT3SH2结构域直接结合，抑制肿瘤细胞⽣长和诱导肿瘤细胞的凋亡(apoptosis)[1]。IC50&TargetSTAT35.18μM(IC50)体外研究STAT3-IN-10(A11)(48h)showsIC50valuesof0.67,0.77,1.24µMagainstMDA-MB-231,MDA-MB-468,HepG2cells,respectively[1].STAT3-IN-10(A11)directlybindstotheSTAT3SH2domain[1].STAT3-IN-10(A11)(0-3μM,24h)inhibitsthephosphorylationofSTAT3anditsdownstreamtargetproteinsandhasagoodselectivityagainstthetumorsuppressorSTAT1[1].STAT3-IN-10(A11)(0-4μM,24h)inducesapoptosisincancercells[1].STAT3-IN-10(A11)(0-4μM,24h)dose-dependentlycausesasignificantSphasearrestinMDA-MB-231cells[1].CellViabilityAssay[1]CellLine:Breastcancercelllines:MDA-MB-231andMDA-MB-468;humanlivercarcinomacellline:HepG2.Concentration:IncubationTime:48h,re-incubatedfor4h(MDA-MB-468,MDA-MB-231)and1h(HepG2).1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:ShowedIC50valuesof0.67,0.77,1.24µMagainstMDA-MB-231,MDA-MB-468,HepG2cells,respectively.WesternBlotAnalysis[1]CellLine:MDA-MB-231.Concentration:0,0.75,1.5and3.0μM.IncubationTime:24h.Result:DecreasedtheSTAT3-Y705phosphorylationwithoutaffectingthetotalamountofSTAT3proteinanddecreasedtheexpressionofSTAT3targetgenes,includingC-MycandCyclinD1inadose-dependentmanner.HadlittleimpactonthelevelofSTAT1anditsphosphorylationonTyr701.ApoptosisAnalysis[1]CellLine:MDA-MB-231.Concentration:0,1,2,and4μM.IncubationTime:24h.Result:InducedtheapoptosisinMDA-MB-231cellsinaconcentration-dependentmannerCellCycleAnalysis[1]CellLine:MDA-MB-231.Concentration:0,1,2,and4μM.IncubationTime:24h.Result:Coulddose-dependentlycauseasignificantSphasearrestinMDA-MB-231cells体内研究STAT3-IN-10(A11)(i.p.;5,10mg/kg;onceaday,21days)inhibitsthegrowthofhumanxenografttumorinvivo[1].AnimalModel:FiveweeksoldfemaleBALB/cnudemice(16–18g)bearinginoculationofhumanbreastcancercellsMDA-MB-231[1].Dosage:5and10mg/kgAdministration:IP,onceaday,21daysResult:Inhibitedthegrowthofhumanxenografttumorinvivowithoutapparentbody-weightloss2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEfortreatedmiceandinhibitedthelevelsofp-STAT3intumortissues.REFERENCES[1].Kai-RuiFeng,etal.Design,synthesisandbiologicalevaluationofnovelpotentSTAT3inhibitorsbasedonBBI608forcancertherapy.EurJMedChem.2020Sep1;201:112428.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedi