DC-PRC2in-01-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDC-PRC2in-01Cat.No.:HY-178694CASNo.:120430-77-5分⼦式:C₂₇H₂₉FN₄O分⼦量:444.54作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性DC-PRC2in-01⼀种强效的EZH2-EED相互作⽤抑制剂，其IC50为4.21μM，Kd为4.56μM。DC-PRC2in-01破坏PRC2复合体的稳定性，导致PRC2核⼼蛋⽩降解和H3K27me3⽔平降低，从⽽抑制PRC2驱动的淋巴瘤细胞增殖并导致细胞周期阻滞。DC-PRC2in-01可⽤于研究PRC2相关的癌症，如弥漫性⼤B细胞淋巴瘤(DLBCL)和滤泡性淋巴瘤(FL)[1]。IC50&TargetEZH2体外研究DC-PRC2in-01(3days)suppressesproliferationofDLBCLcelllines(Pfeiffer,SU-DHL-4,KARPAS-422,andDBcells)withIC50valuesof3.77,5.97,5.87,and9.62μM,respectively.[1].DC-PRC2in-01(0.625-5μM,2-3days)dose-dependentlyinducesG0/G1phasecellcyclearrestsinPfeifferandSU-DHL-4cells[1].DC-PRC2in-01(0-10μM,3days)specificallyinhibitsthePRC2activitybydisruptingtheEZH2-EEDinteraction,leadingtothedepletionofPRC2corecomponentsinPfeiffercells,resultinginadose-dependentdecreaseofH3K27me3levels[1].CellCycleAnalysis[1]CellLine:PfeifferandSU-DHL-4cellsConcentration:0.625,1.25,2.5,and5μMIncubationTime:2daysforPfeiffer,3daysforSU-DHL-4cellsResult:Dose-dependentlyinducedG0/G1phasecellcyclearrestinPfeifferandSU-DHL-4cells1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEwithaconcurrentdecreaseofcellsinG2/MandS.ledtoanincreaseofcellsintheG0/G1phaseat5μMfrom52.3to76.2%andfrom62.2to84%forPfeifferandSU-DHL-4cells,respectively.ResultedinadecreaseofPfeiffercellsinG2/MandSphasesfrom14.9to6.2%andfrom32.8to17.6%,andadecreaseofSU-DHL-4cellsinG2/MandSphasesfrom8.6to0%andfrom29.2to16%.WesternBlotAnalysis[1]CellLine:PfeiffercellsConcentration:0,0.6,1.3,2.5,5,and10μMIncubationTime:3daysResult:Causedadose-dependentlossofH3K27me3,whichvirtuallydisappearedat10μM.DidnotsignificantlyaffecttheotherhistoneH3trimethylationmarks(H3K4me3,H3K9me3,H3K36me3),suggestingitsspecificinhibitionofPRC2activity.REFERENCES[1].DuD,etal.Structure-GuidedDevelopmentofSmall-MoleculePRC2InhibitorsTargetingEZH2-EEDInteraction.JMedChem.2021;64(12):8194-8207.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc