Ferroptosis-inducer-13-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEFerroptosisinducer-13Cat.No.:HY-179481CASNo.:3085517-19-4分⼦式:C₂₁H₂₃NO₃分⼦量:337.41作⽤靶点:Ferroptosis;Keap1-Nrf2;GlutathionePeroxidase;ReactiveOxygenSpecies(ROS)作⽤通路:Apoptosis;NF-κB;MetabolicEnzyme/Protease;Immunology/Inflammation储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Ferroptosisinducer-13⼀种5′-异戊⼆烯化的查尔酮衍⽣物，它通过改变Nrf2/xCT/GPX4通路活性，有效诱导⼈⾮⼩细胞肺癌(NSCLC)细胞发⽣铁死亡(ferroptosis)。Ferroptosisinducer-13在体外表现出强效的抗增殖作⽤，并在NSCLC⼩⿏模型中抑制肿瘤⽣长。Ferroptosisinducer-13可⽤于NSCLC的研究[1]。IC50&TargetGPX4体外研究Ferroptosisinducer-13(compound4a)(72h)exhibitspotentbroad-spectrumantiproliferativeactivityagainstcancercells,withIC50valuesof2.11μM(PC9),2.17μM(MDA-MB-231),3.81μM(SMMC-7721),and4.10μM(SGC-7901)[1].Ferroptosisinducer-13(0-40μM;24-72h)exhibitssignificantanti-proliferativeeffectsonNSCLCcells(PC9andH1975)inatime-andconcentration-dependentmanner[1].Ferroptosisinducer-13(20μM;24h)inducesferroptosisinNSCLCcells(PC9andH1975)[1].Ferroptosisinducer-13(0-40μM;24h)leadstoGSHdepletionandincreasesFe2+,ROSandLPOlevels,andinducesferroptosisthroughmodulationoftheNrf2/xCT/GPX4signalingpathwayinPC9andH1975cells[1].CellViabilityAssay[1]CellLine:PC9,H1975Concentration:0,2.5,5,10,20,40μM1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:24,48,72hResult:GraduallydecreasedcellviabilityofPC9andH1975cellsinaconcentrationmanner.Exhibitedsignificantanti-proliferativeeffectsonNSCLCcells(PC9andH1975)inatime-andconcentration-dependentmanner.CellViabilityAssay[1]CellLine:PC9,H1975Concentration:20μMIncubationTime:12hResult:Significantlyenhancedcellviabilitybyapproximately20%whencombinedwithferroptosisinhibitor.Immunofluorescence[1]CellLine:PC9,H1975Concentration:20μMIncubationTime:24hResult:ModeratelyreversedtheGPXexpressionwhencombinedwithferroptosisinhibitor.WesternBlotAnalysis[1]CellLine:PC9,H1975Concentration:0,5,10,20,40μMIncubationTime:24hResult:SignificantlydecreasedNrf2levelsinbothcytoplasmicandnuclearfractionswhilereducingxCTandGPX4expression.体内研究Ferroptosisinducer-13(2and5mg/kg;i.p.;every3daysfor18days)suppressestumorgrowthinaPC9xenograftmousemodelwithfavorablesafetyprofiles[1].AnimalModel:FemaleBalb/cnudemice(16-20g)subcutaneouslyinjectedwithPC9cells[1]Dosage:2,5mg/kgAdministration:i.p.;every3daysfor18daysResult:Exhibitedtumorgrowthsuppressionwithminimalimpactonbodyweight.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECausednosignificantorgantoxicityinmice.SignificantlydownregulatedtheproteinexpressionofxCTandGPX4intumortissuescomparedwiththecontrolgroup.REFERENCES[1].ZhaoL,etal.Design,synthesisandstructure-activityrelationshipof5'-prenylatedchalconederivativesinhibitedtheproliferationofhumannon-smallcelllungcancercellsviainducingferroptosis.BioorgChem.2025;166:109135.McePdfHeightCaution:Producthasnotbeenfullyva