TED-347-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemETED-347Cat.No.:HY-125269CASNo.:2378626-29-8分⼦式:C₁₅H₁₁ClF₃NO分⼦量:313.7作⽤靶点:YAP作⽤通路:StemCell/Wnt储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(796.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1878mL15.9388mL31.8776mL5mM0.6376mL3.1878mL6.3755mL10mM0.3188mL1.5939mL3.1878mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(19.92mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TED-347⼀种有效，不可逆且共价的YAP-TEAD蛋⽩质-蛋⽩质相互作⽤变构抑制剂，对TEAD4·Yap1蛋⽩1/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE质-蛋⽩质相互作⽤的EC50为5.9μM。TED-347与TEAD4中央⼝袋内的Cys-367特异性共价结合，Ki为10.3μM。TED-347可以阻断TEAD的转录活性，并且具有抗肿瘤活性。IC50&TargetIC50:5.9μM(TEAD4⋅Yap1protein-proteininteraction)[1]体外研究TED-347(0.5-100μM;48hours)inhibitsGBM43cancercellviability[1].TED-347(5μM;48hours)inhibitsco-immunoprecipitationofMyc-taggedTEAD4withFLAG-taggedYap1[1].TED-347(10μM;48hours)showsasignificantreductioninCTGFtranscriptlevels[1].TED-347(0.5-100μM;24hours)reducesreporteractivityincellstransfectedwithaTEADreporter.TED-347(0.5-100μM)alsoinhibitsTEAD4transcriptionalactivityinGBM43cells[1].TED-347isselectiveforTEADsandinhibitsTEAD2withthesameefficacy.TED-347(0.1-100μM;24-48hours)inhibitsTEAD4bindingtofull-lengthYap1indose-andtime-dependentmanner.TED-347(1-100μM)showsnoinhibitionofuPAR•uPAorCav2.2α•βprotein-proteininteractions.Non-covalentbindingofTED-347toTEAD4exhibitslittlechangetotheTEAD4•Yap1bindingaffinity[1].TED-347hasthemaximumrateofinactivationof0.038hours,correspondingtoat1/2∞of18.2hours[1].CellViabilityAssay[1]CellLine:GBM43glioblastomacelllinesConcentration:0.5,1,10,100μMIncubationTime:48hoursResult:InhibitedGBM43cancercellviabilityandinhibitedGBM43cellviabilityby30%at10μM.WesternBlotAnalysis[1]CellLine:HEK-293cellsConcentration:5μMIncubationTime:48hoursResult:Showedasignificantlossofco-immunoprecipitationofMyc-taggedTEAD4withFLAG-taggedYap1.RT-PCR[1]CellLine:HEK-293cellsConcentration:10μMIncubationTime:48hoursResult:ShowedasignificantreductioninCTGFtranscriptlevelsversuscontrolcellsandhadnoinhibitiononTEADmutanttranscriptionalactivityandprotein-proteininteractionsincell2/3MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEculture.REFERENCES[1].KhuchtumurBum-Erdene,etal.Small-MoleculeCovalentModificationofConservedCysteineLeadstoAllostericInhibitionoftheTEADMcePdfHeightCaution:Producthasnotbeenfullyvalidatedform