CARM1-IN-4-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemECARM1-IN-4Cat.No.:HY-161334CASNo.:2878481-07-1分子式:C₂₄H₄₂N₂O₄分子量:422.6作用靶点:HistoneMethyltransferase;Apoptosis作用通路:Epigenetics;Apoptosis储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性CARM1-IN-4(compound11f)是一种有效的CARM1抑制剂，对CARM1和PRMT1的IC50值分别为9nM和56nM。CARM1-IN-4对结直肠癌细胞系显示出显着的抗增殖作用。CARM1-IN-4有效抑制CARM1的甲基转移酶活性，防止下游蛋白甲基化。CARM1-IN-4诱导细胞凋亡，并显示出抗肿瘤活性。IC50&TargetCARM1PRMT1PRMT6PRMT89nM(IC50)56nM(IC50)30nM(IC50)31nM(IC50)PRMT3PRMT52637nM(IC50)>100,000nM(IC50)体外研究CARM1-IN-4(compound11f)exhibitssignificantanti-proliferativeactivityintheHCT116celllines(IC50=3.13μM)[1].CARM1-IN-4(0.625-5μM;72h)causesadose-dependentinductionofapoptosisinHCT116cell[1].CARM1-IN-4(0.625-10μM;48h)effectivelyinhibitsthemethyltransferaseactivityofCARM1,influencingthelevelsofasymmetricdemethylationonCARM1substrateswithinacellularenvironment[1].CARM1-IN-4exhibitsarelativelyhighmitochondrialstability,withanextendedhalf-lifeinmousemitochondria(T1/2=217min)[1].ApoptosisAnalysis[1]CellLine:HCT116cellsConcentration:0.625,1.25,2.5,5μM1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:72hResult:Illustratedanoticeableincreaseintheoverallpercentagesofbothearlyandlateapoptoticcells.WesternBlotAnalysis[1]CellLine:HCT116cellsConcentration:0.625,1.25,2.5,5,10μMIncubationTime:48hResult:Causeddose-dependentreductionsinglobalasymmetricdimethylarginine(aDMA)andasymmetricdimethyl-PABP1levelsinHCT116cells.体内研究CARM1-IN-4(compound11f;10,25mg/kg/day;ip;for12days)showsevidentinhibitoryeffectinBALB/cnudemicebearingsubcutaneousHCT116xenograft[1].AnimalModel:6to8-week-oldfemaleBALB/cnudemicebearingsubcutaneousHCT116xenograft[1]Dosage:10,25mg/kgAdministration:Intraperitonealinjection;daily;for12daysResult:Showedevidentinhibitoryeffect.REFERENCESChenyuLiu,etal.Structure-baseddiscoveryofpotentCARM1inhibitorsforcolorectalcancertherapy.EurJMedChem.2024Mar4:269:116288.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse