OPN-9643-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOPN-9643Cat.No.:HY-179559CASNo.:2866423-06-3分⼦式:C₁₉H₁₆F₃NO₂分⼦量:347.33作⽤靶点:YAP作⽤通路:StemCell/Wnt储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性OPN-9643⼀种针对TEADs中央棕榈酰结合⼝袋的共价抑制剂，IC50为15nM，可防⽌⾃棕榈酰化并降低TEAD-驱动的荧光素酶活性和经典TEAD靶因，如CTGF和CYR61。OPN-9643可⽤于癌症的研究，如⿊⾊素瘤。IC50&TargetTEAD15nM(IC50)体外研究OPN-9643(2ꢀµM;24-48h)reducestheexpressionofTEADtargets(CTGFandCYR61)inSOX10KOcells.OPN-9643reducesluciferaseactivity.OPN-9643reducesotherknownTEADtargets,suchasDKK1,MYC,andTGF-β2inSOX10KOmelanomacells[1].\nOPN-9643(NCI-H226cells;5days)inhibitsTEADactivityandcellgrowth(IC50of123nM)inNCI-H226cells[1].WhenadministeredincombinationwithBRAFi(BRAFinhibitor)+MEKi(MEKinhibitor),andOPN-9643(2μM;48-72h)markedlydecreasescellgrowthinA375SOX10KOcellscomparedtoBRAFi+MEKialone[1].OPN-9643(2μM;48h)increasesthecleaved-PARPandcleaved-GSDMEinthecombinationtreatedSOX10KOcells[1].WesternBlotAnalysis[1]CellLine:A375parental,A375crSOX10#2.18,andA375crSOX10#4.21cellsConcentration:2μMIncubationTime:24h,48h1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:WesternblottinganalysisdetectedareductioninCTGFandCYR61proteinexpressioninSOX10KOcells.Down-regulatedthecellcycleprogressionregulators(FOXM1andPLK1),growthfactorreceptors(phospho-cMETY1234/5,AXL),aserineproteaseinhibitor(PAI1),andRAD51.REFERENCES[1].OttCA,etal.TargetingTAZ-TEADinminimalresidualdiseaseenhancesthedurationoftargetedtherapyinmelanomamodels.NatCommun.2025;16(1):9655.Published2025Nov5.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-379