GPX4-IN-20-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGPX4-IN-20Cat.No.:HY-178389分⼦式:C₃₀H₃₀ClNO₈分⼦量:568.01作⽤靶点:MolecularGlues;GlutathionePeroxidase;Ferroptosis;ReactiveOxygenSpecies(ROS)作⽤通路:PROTAC;Apoptosis;MetabolicEnzyme/Protease;Immunology/Inflammation;NF-κB储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性GPX4-IN-20⼀种Arctigenin(HY-N0035)衍⽣物，GPX4的分⼦胶(molecularglue)降解剂，并通过增加脂质ROS⽔平和抑制GSH⽔平来诱导铁死亡(ferroptosis)。GPX4-IN-20以剂量依赖性⽅式降低GPX4的蛋⽩质表达和酶活性，⽽不响其他与铁死亡相关的蛋⽩质。GPX4-IN-20可诱导GPX4的泛素化依赖性蛋⽩酶体降解。GPX4-IN-20还增加了HCT-116细胞中丙⼆醛(MDA)的⽔平。GPX4-IN-20可⽤于结直肠癌的研究[1]。体外研究GPX4-IN-20(compoundW25)(2.5-10μM;24-72h)showscytotoxicactivityonHCT-116cells[1].GPX4-IN-20(2.5-10μM;24hours;HCT-116cells)inhibitsGPX4proteinexpressionandactivity,promotingubiquitination-dependentproteasomaldegradation.GPX4-IN-20hasnosignificanteffectonotherkeyregulatoryfactorsofferroptosis,suchasferroptosissuppressorprotein1(FSP1),ferritinheavychain1(FTH1),nuclearreceptorcoactivator4(NCOA4),andsolutecarrierfamily7member11(SLC7A11)[1].GPX4-IN-20(2.5-10μM;24hours;HCT-116cells)doesnotaffectGPX4mRNAlevels[1].GPX4-IN-20(0,2.5,5,10μM;6h)inhibitsthecloneformationofHCT-116cellsinadose-dependentmanner[1].GPX4-IN-20(24h)inhibitsthecellgrowthofHT-29withanIC50of4.60μM[1].GPX4-IN-20(0,2.5,5,10μM;6,12,24hours;HCT-116cells)significantlyincreasesthelipidROSlevelsinHCT-116cellswithadose-andtime-dependentmanner.GPX4-IN-20significantlydecreasesGPX4levels.AftertreatmentwithGPX4-IN-20,intracellularMDAcontentisincreasedinadose-dependentmanner[1].CellProliferationAssay[1]CellLine:HCT-116cellsConcentration:0,2.5,5,10μM1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:24hours,48hours,72hoursResult:AfterHCT-116cellsweretreatedfor24,48,and72h,theresultingIC50valueswere4.17μM,2.49μM,and2.24μM,respectively.WesternBlotAnalysis[1]CellLine:HCT-116cellsConcentration:0,2.5,5,10μMIncubationTime:24hoursResult:InhibitedtheproteinexpressionofGPX4inadose-dependentmanner;suppressedtheactivityofGPX4;promotedtheubiquitinationlevelofGPX4,inducingubiquitination-dependentproteasomaldegradationofGPX4.RealTimeqPCR[1]CellLine:HCT-116cellsConcentration:0,2.5,5,10μMIncubationTime:24hoursResult:DidnotsignificantlyaffectGPX4mRNAlevelsinHCT-116cells.REFERENCES[1].WangYX,etal.Design,synthesis,andbiologicalevaluationofarctigeninderivativesasnovelGPX4inhibitorsincolorectalcancercells.EurJMedChem.2025;300:118181.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala