SR-0813-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESR-0813Cat.No.:HY-145409CASNo.:2597186-19-9分⼦式:C₂₅H₃₂N₆O₃S分⼦量:496.62作⽤靶点:EpigeneticReaderDomain作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性SR-0813⼀种有效的选择性ENL/AF9YEATS结构域抑制剂。SR-0813对于ENLYEATS结构域的IC50和EC50值分别为25nM和205nM。SR-0813对于AF9YEATS结构域的IC50和EC50值分别为311nM和76nM(CETSA)。SR-0813结合MAP3K19的亲和⼒(Kd=3.5μM)⽐ENLYEATS(Kd=30nM)低100倍以上。SR-0813可⽤于急性⽩⾎病的研究[1]。IC50&TargetENLYEATSdomainENLYEATSdomainAF9YEATSdomainAF9YEATSdomain25nM(IC50)205nM(EC50)311nM(IC50)76nM(EC50)ENLYEATSdomainMAP3K1930nM(Kd)3.5μM(Kd)体外研究SR-0813(compound10;0,1,10μM;4h)dose-dependentevictsENLfromknownENLbindingsites,includingtheHOXA10genebodyandMYBpromoterinMV4;11cells[1].SR-0813(0,1,10μM;0,24,48,72h)downregulatesthetranscriptlevelsofHOXA9,MEIS1,andMYC,andincreasestheabundanceoftheITGAMtranscriptinMV4;11cells[1].SR-0813(0,1,10μM;approximately2weeks)inhibitsthegrowthofmultiplelineageleukemia(MLL)-fusionleukemiacelllines(MV4;11,MOLM-13,OCI/AML-2)andHB11;19cells[1].SR-0813(1μM,4h)doesnotelicitglobalchangesingeneexpressioninMV4;11cells,butproducesastrikinglyselectivesuppressionofENLtargetgenes[1].CellProliferationAssay[1]CellLine:MLL-fusionleukemiacelllines:MV4;11(MLL-AF4AML),MOLM-13(MLL-AF9AML),and1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEOCI/AML-2(MLL-AF6AML),whicharesensitivetothegeneticlossofENL.HB11;19cells,whichharboringanMLL-ENLfusion.Concentration:0,1,10μMIncubationTime:Approximately2weeksResult:Inhibitedthegrowthofcells.REFERENCES[1].Garnar-WortzelL,etal.ChemicalInhibitionofENL/AF9YEATSDomainsinAcuteLeukemia.ACSCentSci.2021May26;7(5):815-830.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:40