MC3817-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMC3817Cat.No.:HY-179409分⼦式:C₃₃H₄₁Cl₄N₉O分⼦量:721.55作⽤靶点:DNAMethyltransferase;Caspase;MDM-2/p53;DNA/RNASynthesis;Apoptosis作⽤通路:Epigenetics;Apoptosis;CellCycle/DNADamage储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性MC3817⼀种选择性DNMT抑制剂。MC3817对DNMT1和DNMT3A/3L的IC50值分别为0.044μM和>10μM。MC3817可抑制P53依赖性的癌细胞增殖，诱导细胞凋亡和DNA损伤，并提⾼cleavedCaspase3、P53与γH2AX的⽔平。MC3817可⽤于⾮⼩细胞肺癌、结肠癌、宫颈癌、三性乳腺癌以及组织细胞淋巴瘤的相关研究[1]。IC50&TargetDNMT1DNMT3a/3L0.044μM(IC50)>10μM(IC50)体外研究MC3817(compound14)(0.05-100μM,48h)exhibitsantiproliferativeactivityagainstA549andH460(non-smallcellandlungcancer),HCT-116(coloncancer),HeLa(cervicalcancer),MDA-MB-231(triple-negativebreastcancer),andU937(histiocyticlymphoma)cells[1].MC3817(2μM,24and48h)inducesS/G2MphasearrestandtriggersapoptoticcelldeathinHCT-116cells[1].MC3817(0.5-5μM,16-48h)triggersDNAdamageandactivatesthep53/γH2AXpathway,leadingtocell-cyclearrestandapoptosisinHCT116cells[1].MC3817(2.5μM,48h)inducesamuchhigherlevelofapoptosisinHCT-116P53WTcellscomparedwithHCT-116P53−/−cells[1].CellViabilityAssay[1]CellLine:A549,H460,HCT-116,HeLa,MDA-MB231,andU937Concentration:0.05-100μM1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:48hResult:HadIC50of5.5μM,6.8μM,0.4μM,4.2μM,1.9μMand5.5μMforA549cells,H460cells,HCT-116cells,HeLacells,MDA-MB231cells,andU937cells.CellCycleAnalysis[1]CellLine:HCT-116cellsConcentration:2μMIncubationTime:48hResult:CausedablockintheS/G2Mphaseassociatedwithapoptoticcelldeath,affectingover50%ofthecellsafter48h.WesternBlotAnalysis[1]CellLine:HCT-116cellsConcentration:0.5,1,2.5,5μMIncubationTime:48hResult:InducedtheaccumulationofγH2AXandelevatedp53levels,indicatingp53stabilizationandactivationinresponsetoDNAdamage.ApoptosisAnalysis[1]CellLine:HCT-116P53−/−cellsandHCT-116P53WTcells.Concentration:2.5μMIncubationTime:48hResult:Inducedapoptoticcelldeath,asevidencedbysignificantPI/AnnexinVfluorescenceandextensivemembraneblebbinginbothcelllines.REFERENCES[1].ZwergelC,etal.Quinoline-BasedDNAMethyltransferaseInhibitorsFeaturingBasicSideChains:Design,Synthesis,andInsightinBiochemicalandAnticancerCellProperties.JMedChem.2025Nov27;68(22):23886-23909.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications