Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACERRαDegrader-3Cat.No.:HY-139185CASNo.:2306388-65-6分?式:C??H??F?N?O?S分?量:956.99作?靶點:PROTACs;EstrogenReceptor/ERR作?通路:PROTAC;Others儲存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:80mg/mL(83.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.0449mL5.2247mL10.4494mL5mM0.2090mL1.0449mL2.0899mL10mM0.1045mL0.5225mL1.0449mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2mg/mL(2.09mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性PROTACERRαDegrader-3?種于vonHippel-Lindau配體的強效選擇性ERRα降解劑。PROTACERRαDegrader-3能夠在30nM的濃度下將ERRα蛋?特異性降解>80%。PROTACERRαDegrader-3對ERRβ和ERRγ蛋??活性。IC50&TargetERRαVHL體外研究PROTACERRαDegrader-3(compound6c;0.3nM-10μM;4hours)dose-dependentlyinducesERRαdegradationwithanefficaciousdoseaslowas3.0nMat4.0h.PROTACERRαDegrader-3potentlydecreasesproteinlevelsofERRαdownstreamtargetgenes,e.g.,ATP5B,medium-chainacylCoAdehydrogenase(MCAD),andpyruvatedehydrogenasekinase4(PDK4)intheMDA-MB-231cellsaftera24htreatment[1].PROTACERRαDegrader-3exhibitsanIC50valueof12.67nMtoblocktheprotein-proteininteractionofERRαwithPGC-1αpeptideandinducesapproximately96%proteindegradationat100nM(D100nM)after4.0htreatment[1].WesternBlotAnalysis[1]CellLine:MDA-MB-231cellsConcentration:0.3nM,1nM,3nM,10nM,30nM,100nM,300nM,1μM,3μM,10μMIncubationTime:4hoursResult:Dose-dependentlyinducedERRαdegradation.REFERENCES[1].LijiePeng,etal.IdentificationofNewSmall-MoleculeInducersofEstrogen-relatedReceptorα(ERRα)Degradation.ACSMedChemLett.2019Apr12;10(5):767-772.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseo