Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemESTAT3/CAIX-IN-1Cat.No.:HY-174457CASNo.:3053583-60-8分子式:C??H??F?N?O?S?分子量:687.63作用靶點(diǎn):STAT;CarbonicAnhydrase;Ferroptosis;Apoptosis;ReactiveOxygenSpecies(ROS);Caspase;Bcl-2Family作用通路:JAK/STATSignaling;StemCell/Wnt;MetabolicEnzyme/Protease;Apoptosis;Immunology/Inflammation;NF-κB儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性 STAT3/CAIX-IN-1是STAT3(Kd：60.03μM)和CAIX(IC50：80.45nM)的雙靶點(diǎn)抑制劑。STAT3/CAIX-IN-1通過(guò)增加活性氧(ROS)和脂質(zhì)過(guò)氧化物的水平來(lái)誘導(dǎo)鐵死亡(ferroptosis)。STAT3/CAIX-IN-1抑制細(xì)胞遷移，誘導(dǎo)細(xì)胞凋亡(apoptosis)，并導(dǎo)致MDA-MB-231細(xì)胞周期停滯。STAT3/CAIX-IN-1可用于三陰性乳腺癌(TNBC)的研究[1]。IC50&TargetCAIXhCAVBhCAIISTAT380.45nM(IC50)25.40nM(IC50)349.30nM(IC50)60.03μM(Kd)體外研究STAT3/CAIX-IN-1(Compound7m)(2-8μM,24h)inhibitsSTAT3phosphorylationinMDA-MB-231cells[1].STAT3/CAIX-IN-1(4μM)bindstoSTAT3toenhanceitsstability[1].STAT3/CAIX-IN-1enhancesproliferationinhibitionoftumorcelllineswithIC50sof2.18μM(hypoxia)and4.21μM(normoxia)intheMDA-MB-231cellline[1].STAT3/CAIX-IN-1(4μM,8μM,24h)inducesferroptosisviatheGPX4pathway,increasesreactiveoxygenspecies(ROS)levels,upregulatesintracellularlipidperoxidationinMDA-MB-231cells[1].STAT3/CAIX-IN-1(2μM,4μM,24-48h)inhibitsthemigrationofMDA-MB-231cells[1].STAT3/CAIX-IN-1(4μM,8μM,24h)inducesapoptosisinMDA-MB-231cells,inducescellcyclearrestinMDA-MB-231cellsattheG1/Sphase[1].STAT3/CAIX-IN-1hasanti-tumoractivitywithIC50sof4.21μM(MDA-MB-231),5.67μM(MCF-7),6.60μM(MDA-MB-231/ADR),14.19μM(MCF-10A)[1].WesternBlotAnalysis[1]1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:MDA-MB-231cellsConcentration:2,4,8μMIncubationTime:24hResult:InhibitedthelevelsofpSTAT3-S727andpSTAT3-Y705.Nochangedp-JAK1levels.ReducedGPX4levels.DownregulatedtheexpressionofBcl-2andCyclinD1.CellCycleAnalysis[1]CellLine:MDA-MB-231cellsConcentration:4,8μMIncubationTime:24hResult:AccumulatedinG1phasecells,downregulatedSphasecells.ApoptosisAnalysis[1]CellLine:MDA-MB-231cellsConcentration:4,8μMIncubationTime:24hResult:InducedapoptosisinMDA-MB-231cells.CellMigrationAssay[1]CellLine:MDA-MB-231cellsConcentration:2,4,8μMIncubationTime:24h,48hResult:Reducedmobility.體內(nèi)研究STAT3/CAIX-IN-1(Compound7m)(5mg/kg,10mg/kg,48h)showsanti-tumoractivitywith75%TIR,notchangesweightorbehavior[1].STAT3/CAIX-IN-1(10mg/kg,i.p.,21days,every2days)reducesphosphorylatedSTAT3expressioninBalb/cnudemousexenograftexperiments[1].STAT3/CAIX-IN-1(5mg/kg,10mg/kg,i.p.,21days,every2days)inhibitstumorgrowthonBalb/cnudemicewithMDA-MB-231xenografttumors[1].2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEAnimalModel:Balb/cnudemicewithMDA-MB-231xenografttumors[1].Dosage:10mg/kgAdministration:i.p.,21days,every2daysResult:ReducedthefluorescenceintensityofpSTAT3-S727(greenfluorescence)andpSTAT3-Y705(redfluorescence).REFERENCESChenL,etal.DiscoveryofDiarylPiperidone-SulfonamideasaNovelDual-TargetInhibitorofSTAT3/CAIXInducingFerroptosisinTriple-NegativeBreastCancerCells.JMedChem.2025Jun26;68(12):12493-12512.McePdfHeightCaution:Producthasnotbeenf