Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemETS-IN-8Cat.No.:HY-178911分子式:C??H??FN?O?S分子量:389.44作用靶點:ThymidylateSynthase;Apoptosis;ReactiveOxygenSpecies(ROS);Bcl-2Family;Caspase作用通路:Apoptosis;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性TS-IN-8是一種強效的胸苷酸合成酶(TS)抑制劑。TS-IN-8可誘導MCF-7細胞凋亡(apoptosis)，并導致細胞周期停滯于G2/M期。TS-IN-8可誘導細胞核形態(tài)改變。TS-IN-8可增加細胞內(nèi)活性氧(ROS)水平。TS-IN-8可通過調(diào)節(jié)凋亡相關(guān)蛋白(如bax/bcl-2比值和caspase活化)激活內(nèi)源性凋亡通路。TS-IN-8可用于乳腺癌的研究[1]。體外研究TS-IN-8(Compound4d)(1-80μM,24h)showsstronginhibitoryeffectsonMCF-7cells(IC50=10.11μM)andA549cells(IC50=22.49μM),weakerinhibitoryeffectsonHepG2cells,andlowtoxicitytonormalMcCoycells(IC50=115.86μM)[1].TS-IN-8(1-5μM,24h)inducesapoptosisinMCF-7cellsinadose-dependentmannerandcausescellcyclearrestattheG2/Mphase[1].TS-IN-8(1-5μM,24h)inducesdose-dependentnuclearmorphologicalchangesinMCF-7cells,includingchromatincondensationat1μM(apoptoticnuclearindex4.12%)andnuclearfragmentationwithapoptoticbodiesat5μM(apoptoticnuclearindex8.97%),significantlyincreasesintracellularreactiveoxygenspecies(ROS)levels,andactivatesintrinsicapoptosispathwaysbyregulatingapoptosis-relatedproteinssuchasbax/bcl-2ratioandCaspaseactivation[1].TS-IN-8(1-5μM,6h)significantlyreducesTSproteinexpressioninMCFcells[1].TS-IN-8(1-5μM,24h)inhibitsMCF-7cellmigrationinadose-dependentmanner[1].TS-IN-8(1-5μM,24h)disruptsthestructuralintegrityof3Dtumorspheresandreducesthenumberoflivecellswhileincreasingtheproportionofdeadcellsin3Dspheres[1].CellCytotoxicityAssay[1]CellLine:MCF-7cells,A549cells,HepG2cells,McCoycells1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:1μM,5μM,10μM,20μM,40μM,60μM,80μMIncubationTime:24hResult:ShowedstronginhibitoryeffectsonMCF-7cells(IC50=10.11μM)andA549cells(IC50=22.49μM),weakerinhibitoryeffectsonHepG2cells,andlowtoxicitytonormalMcCoycells(IC50=115.86μM).ApoptosisAnalysis[1]CellLine:MCF-7cellsConcentration:1μM,5μMIncubationTime:24hResult:At1μM,theproportionofapoptoticcellsincreasedto3.27%;at5μM,theproportionofapoptoticcellsincreasedto6.49%.CellCycleAnalysis[1]CellLine:MCF-7cellsConcentration:1μM,5μMIncubationTime:24hResult:At1μM,thepercentageofcellsintheG2/Mphaseincreasedto34.8%;at5μM,thepercentageofcellsintheG2/Mphaseincreasedto39.8%.WesternBlotAnalysis[1]CellLine:MCF-7cellsConcentration:1μM,5μMIncubationTime:24hResult:Pro-apoptoticproteinBaxexpressionwasupregulated,whileanti-apoptoticproteinsBcl-2andSurvivinexpressionweredownregulated.ThecleavagepatternsofCaspase-3,Caspase-9,andPARP-1wereincreased.AnelevatedBax/Bcl-2ratioindicatesactivationofthemitochondrialpathwayforapoptosis.WesternBlotAnalysis[1]CellLine:MCF-7cells2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEConcentration:1μM,5μMIncubationTime:24hResult:TSproteinexpressionlevelswerereduced(0.8-foldcomparedtothecontrolat1μMand0.6-foldcomparedtothecontrolat5μM).CellMigrationAssay[1]CellLine:MCF-7cellsConcentration:1μM,5μMIncubationTime:24hResult:At1μM,reducedthewoundclosurerateto68.4%;at5μM,reducedthewoundclosurerateto55.6%.REFERENCESJaitakA,etal.Design,synthesis,anticancerevaluation,andInsilicostudiesof2-thiopyrimidine-5-carbonitrilederivativesaspotentthymidylatesynthaseinhibitors.EurJMedChem.2026Jan5;301:118205.McePdfHeightCaution:P