TGFβRII-IN-3-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETGFβRII-IN-3Cat.No.:HY-161398分⼦式:C₂₆H₂₅F₃N₂O₂分⼦量:454.48作⽤靶点:TGF-βReceptor;TGF-beta/Smad作⽤通路:TGF-beta/Smad;StemCell/Wnt储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性TGFβRII-IN-3(Compound2r)⼀种选择性的TGFβ类型II受体(TGFβRII)的抑制剂(IC50=4.1μM)。其通过促进TGFβRII的蛋⽩质降解来抑制TGFβ信号传导。TGFβRI-IN-7可以阻断内⽪向间充质的转变和细胞迁移。TGFβRI-IN-7还能够⽤于癌症研究[1]。IC50&TargetTGF-βR24.1μM(IC50)体外研究TGFβRII-IN-3(5-15μM;24h)inhibitstheactivityoftheTGFβsignalingpathwaybyreducingthephosphorylationlevelsofSmad2inA549cellsanddemonstratesselectivedegradationofTGFβRII[1].TGFβRII-IN-3(2.5-10μM;48h)effectivelyinhibitsthelossofE-cadherininducedbyTGFβ1,whilesuppressingtheupregulationofSnailandN-cadherin[1].TGFβRII-IN-3(5μM;48h)inhibitscellmigrationandmorphologicalchangesbysuppressingTGFβsignalinginA549andH1299cells[1].WesternBlotAnalysis[1]CellLine:A549cellConcentration:5;10;15μMIncubationTime:24hResult:Significantlyanddose-dependentlyinhibitedTGFβ1-inducedphosphorylationofSmad2inA549cells.Significantlyreducedthesteady-statelevelsofTβRIIinadose-dependentmanner.At1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEthesametime,thelevelsofTGFβtypeIreceptorwerenotsignificantlyaffected.REFERENCES[1].LängleD,etal.ExpandingtheChemicalSpaceofTransformingGrowthFactor-β(TGFβ)ReceptorTypeIIDegraderswith3,4-DisubstitutedIndoleDerivatives.ACSPharmacolTranslSci.2024Mar21;7(4):1069-1085.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3792;021-