METTL3-IN-11-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEMETTL3-IN-11Cat.No.:HY-178446CASNo.:3069369-05-4分子式:C₂₆H₂₈N₆O₃分子量:472.54作用靶点:METTL3;c-Myc;Bcl-2Family作用通路:Epigenetics;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性METTL3-IN-11是一种优异的选择性METTL3抑制剂(IC50=45.31nM)。与DNMT1、EZH1、MLL1和PRMT1相比，METTL3-IN-11对METTL3表现出较高的选择性。METTL3-IN-11降低了MOLM-13和SKOV3细胞中总RNA的m6A水平，诱导细胞凋亡(apoptosis)，并抑制细胞迁移。METTL3-IN-11可以降低m6A下游靶基因(c-MYC和BCL2)的表达。METTL3-IN-11可用于卵巢癌和急性髓系白血病的研究[1]。IC50&TargetBcl-2体外研究METTL3-IN-11(Compound30t)exhibitsgoodantiproliferativeactivityinbothSKOV3(IC50=6.42μM)andMOLM-13(IC50=12.34μM)cells,whileshowinglowtoxicityinLO2andHK2cells,withthesurvivalrateofHK2cellsat25μMand50μMbeingsignificantlyhigherthanthatofthepositivecontrolSTM2457[1].METTL3-IN-11(5-15μM)reducesthem6AlevelsontotalRNAinadose-dependentmannerinSKOV3andMOLM-13cells[1].METTL3-IN-11(10-25μM,48h)significantlyinhibitsthemigratorycapabilityofSKOV3cellsandinducesapoptosis[1].METTL3-IN-11(10-25μM,48h)doesnotaffecttheexpressionlevelofMETTL3protein,butitdownregulatestheproteinexpressionofdownstreamtargetgenesofm6A(suchasc-MYCandBCL2)inSKOV3andMOLM-13cellsinadose-dependentmanner[1].CellMigrationAssay[1]CellLine:SKOV3cellsConcentration:10μM,25μM1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:48hResult:SignificantlyinhibitsthemigratorycapabilityofSKOV3cells.WesternBlotAnalysis[1]CellLine:SKOV3cells,MOLM-13cellsConcentration:10μM,25μMIncubationTime:48hResult:DidnotaffecttheexpressionlevelofMETTL3protein.Downregulatedtheproteinexpressionofdownstreamtargetgenesofm6A(suchasc-MYCandBCL2).体内研究METTL3-IN-11(Compound30t)(50mg/kg,i.p.,oncedailyfor2weeks)significantlyinhibitstumorgrowthinmicebearingSKOV3cellsandmaintainsstablebodyweightduringtheexperiment,andnoobvioustoxicreactionsareobserved[1].AnimalModel:SKOV3cellsweresubcutaneouslyinoculatedintotherightflankoffemaleBALB/cmice(4–5weeksold)[1].Dosage:50mg/kgAdministration:I.p.,oncedailyfor2weeksResult:Significantlyinhibitedtumorgrowth.Nosignificantdifferencewasobservedinthebodyweight.REFERENCESMiaoR,etal.Identificationofnovel2,6-Di-substitutedImidazo[1,2-a]pyridinederivativesaspotentMETTL3inhibitors.BioorgChem.2025Oct;165:108980.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications