TED-347-DataSheet-生命科學(xué)試劑-生命科學(xué)試劑-MedChemExpress

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(diǎn):YAP作?通路:StemCell/Wnt儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(796.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.1878mL15.9388mL31.8776mL5mM0.6376mL3.1878mL6.3755mL10mM0.3188mL1.5939mL3.1878mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案，配制前請(qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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(qǐng)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(jià)的YAP-TEAD蛋?質(zhì)-蛋?質(zhì)相互作?變構(gòu)抑制劑，對(duì)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(jià)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