FTO-IN-16-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFTO-IN-16Cat.No.:HY-179267分⼦式:C₂₃H₂₃Cl₂N₃O₆分⼦量:508.35作⽤靶点:FatMassandObesity-associatedProtein(FTO);c-Myc;RAR/RXR;Apoptosis作⽤通路:MetabolicEnzyme/Protease;Apoptosis;VitaminDRelated/NuclearReceptor储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性FTO-IN-16，FTO-IN-15(HY-179266)的前药，⼀种强效FTO抑制剂。FTO-IN-16可抑制急性髓系⽩⾎病(AML)细胞的活⼒，增加m6A⽔平，下调c-Myc和CEBPA的表达，并上调ASB2和RARA的表达。FTO-IN-16诱导细胞凋亡(apoptosis)。FTO-IN-16在AML⼩⿏异种移植模型中显⽰出显著的体内活性。FTO-IN-16可⽤于AML的研究[1]。体外研究FTO-IN-16(0-8μM;48h)downregulatesc-MycandCEBPA(proteinandmRNA),andupregulatesASB2andRARAinmultipleAMLcells(NB4,MOLM13,MV4-11,HEL,OCI-AML3,NOMO-1,KG-1)[1].FTO-IN-16(0-20μM;48h)inducesdose-dependentapoptosisinNB4cells[1].FTO-IN-16(0-8μM;48h)downregulatesc-MycandCEBPA(proteinandmRNA),andupregulatesASB2andRARAinmultipleAMLcells(NB4,MOLM13,MV4-11,HEL,OCI-AML3,NOMO-1,KG-1)[1].FTO-IN-16(72h)exhibitspotentantileukemicactivityacrossapanelofAMLcelllines,withIC50valuesof5.5(NB4),2.3(MOLM13),4.4(KG-1),3.6(MV4-11),4.6(HEL),5.2(OCI-AML3),and4.7μM(NOMO-1),respectively[1].CellViabilityAssay[1]CellLine:MOLM13Concentration:0,2,4,8μMIncubationTime:24,48,72hResult:Inducedtime-dependentgrowthinhibition.Significantlyinhibitedcellgrowthafter72htreatmentat8μMcomparedtothecontrol.1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellProliferationAssay[1]CellLine:NB4Concentration:0,1,2,4μMIncubationTime:7daysResult:Induceddose-dependentsuppressionofcolonyformation.ApoptosisAnalysis[1]CellLine:NB4Concentration:0,5,10,20μMIncubationTime:48hResult:Induceddose-dependentapoptosis.WesternBlotAnalysis[1]CellLine:NB4,MOLM13,MV4-11,HEL,OCI-AML3,NOMO-1,KG-1Concentration:0,2,4,8μMIncubationTime:48hResult:UpregulatedtumorsuppressorsRARAandASB2.ReducedproteinlevelsoftheoncoproteinsCEBPAandc-Myc.Thedownregulationofc-Mycproteinwasconsistentlyobservedacross7testedAMLcelllines.DidnotaltertheproteinlevelsofFTOitselforothermajorm6Aregulators,includingALKBH5andMETTL3.RealTimeqPCR[1]CellLine:NB4Concentration:0,4,8μMIncubationTime:48hResult:IncreasedASB2expressionaccompaniedbydecreasedc-MycandCEBPAtranscripts.体内研究FTO-IN-16(30and60mg/kg;i.p.;dailyfor9days)impairsAMLprogressionthroughm6A-mediatedtranscriptionalregulationinanAMLmousexenograftmodel[1].AnimalModel:FemaleBALB/cnudemicesubcutaneouslyinjectedwithNB4AMLcells[1]Dosage:30and60mg/kg2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:i.p.;dailyfor9daysResult:Significantlysuppressedtumorgrowthinadose-dependentmanner.Showednosignificantbodyweightlossororgantoxicity.Resultedinupregulationoftumorsuppressors(RARA,ASB2)anddownregulationofoncoproteins(CEBPA,c-Myc).ShowedamarkedincreaseinglobalRNAm6Amodifications.REFERENCES[1].HY-179267-FTO-IN-16-compound8a-1.pdfMcePdfHeightCaution:Producthasnotbeenfullyval