Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemETED-347Cat.No.:HY-125269CASNo.:2378626-29-8分?式:C??H??ClF?NO分?量:313.7作?靶點:YAP作?通路:StemCell/Wnt儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(796.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1878mL15.9388mL31.8776mL5mM0.6376mL3.1878mL6.3755mL10mM0.3188mL1.5939mL3.1878mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥6.25mg/mL(19.92mM);ClearsolutionBIOLOGICALACTIVITY?物活性TED-347?種有效，不可逆且共價的YAP-TEAD蛋?質(zhì)-蛋?質(zhì)相互作?變構(gòu)抑制劑，對TEAD4·Yap1蛋?1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE質(zhì)-蛋?質(zhì)相互作?的EC50為5.9μM。TED-347與TEAD4中央?袋內(nèi)的Cys-367特異性共價結(jié)合，Ki為10.3μM。TED-347可以阻斷TEAD的轉(zhuǎn)錄活性，并且具有抗腫瘤活性。IC50&TargetIC50:5.9μM(TEAD4?Yap1protein-proteininteraction)[1]體外研究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?邊的抑制劑?師www.MedChemEculture.REFERENCES[1].KhuchtumurBum-Erdene,etal.Small-MoleculeCovalentModificationofConservedCysteineLeadstoAllostericInhibitionoftheTEADMcePdfHeightCaution:Producthasnotbeenfullyvalidatedform