PROTAC-EED-degrader-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPROTACEEDdegrader-1Cat.No.:HY-130614CASNo.:2639882-72-5分?式:C??H??FN??O?S分?量:1054.2作?靶點(diǎn):PROTACs;HistoneMethyltransferase作?通路:PROTAC;Epigenetics儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:150mg/mL(142.29mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.9486mL4.7429mL9.4859mL5mM0.1897mL0.9486mL1.8972mL10mM0.0949mL0.4743mL0.9486mL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；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。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。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(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，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥3.75mg/mL(3.56mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoil1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:3.75mg/mL(3.56mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性PROTACEEDdegrader-1于vonHippel-Lindau的靶向EED的PROTAC分?，pKD為9.02。PROTACEEDdegrader-1靶向EED亞的多梳抑制復(fù)合物2(PRC2)抑制劑(pIC50=8.17)[1]。IC50&TargetVHL體外研究PROTACEEDdegrader-1(CompoundPROTAC2)bindstoEEDwithapKDof9.02±0.09andinhibitsPRC2functionwithapIC50of8.17±0.24[1].PROTACEEDdegrader-1(0.01-100μM;14days)canpotentlyinhibitproliferationofanEZH2mutantDLBCLcelllineKarpas422[1].PROTACEEDdegrader-1(0.1-3μM;48hours)reducestheproteinlevelsofEED,EZH2,H3K27me3inKarpas422cells[1].PROTACEEDdegrader-1(1μM;1-24h)promotesdegradationofEED,EZH2,andSUZ12inKarpas422cells[1].CellProliferationAssay[1]CellLine:Karpas422cellsConcentration:0.01,0.1,1,10,100μMIncubationTime:4,8,12,14daysResult:Reducedproliferation.GI50=0.045uM(Day14).WesternBlotAnalysis[1]CellLine:Karpas422cellsConcentration:0.1,1,and3μMIncubationTime:48hoursResult:TheproteinlevelsofEED,EZH2,H3K27me3wasreduced.WesternBlotAnalysis[1]CellLine:Karpas422cellsConcentration:1μMIncubationTime:1,2,4,6,8,24hoursResult:EEDproteinlevelsdecreasedwithin1-2hoftreatment.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].HsuJH,etal.EED-TargetedPROTACsDegradeEED,EZH2,andSUZ12inthePRC2Complex.CellChemBiol.2019Nov26.pii:S2451-9456(19)30362-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo