XSJ151-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEXSJ151Cat.No.:HY-179520CASNo.:1685279-23-5分⼦式:C₃₇H₃₁N₅O₁₀S分⼦量:737.73作⽤靶点:Topoisomerase;DNA/RNASynthesis;MDM-2/p53;Bcl-2Family作⽤通路:CellCycle/DNADamage;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性XSJ151⼀种拓扑异构酶I(topoisomeraseI)抑制剂，它能稳定DNA-拓扑异构酶I共价复合物并诱导DNA双链断裂。XSJ151诱导的DNA损伤(DNAdamage)激活p53-p21信号通路，特异性地调控细胞周期蛋⽩的表达，导致G2/M期细胞周期阻滞，并破坏Bcl-2家族蛋⽩的动态稳态，从⽽触发胃癌细胞凋亡(apoptosis)。XSJ151可⽤于胃癌的研究[1]。IC50&TargetTopoisomeraseIBcl-2Bax体外研究XSJ151(48h)exhibitsstrongcytotoxicityagainstgastriccancercelllines,includingAGS(IC50=0.088μM),MGC803(IC50=0.592μM),HGC27(IC50=1.951μM),andSGC7901(IC50=11.121μM),whileshowinglowercytotoxicityagainstnormalcelllinessuchasGES-1(IC50=0.202μM)andHIEC(IC50>40μM)[1].XSJ151(0.1-2.5nM,7-10days)inhibitsgastriccancercellcolonyformationinaconcentration-dependentmanner.InAGScells,2.5nMXSJ151reducesthecolonycountfrom74to22;inMGC803cells,itreducesitfrom68to21[1].XSJ151(2.5-10nM,24h)dose-dependentlyinducesG2/MphasearrestinAGSandMGC803gastriccancercells,leadingtosignificantenrichmentoftheG2/M-phasepopulation[1].XSJ151(44-600nM,48h)significantlyupregulatestheexpressionofG2/Mphase-relatedproteins(p53,p21,CCNB)andtheSphasemarkerCCNAinAGSandMGC803cells,whiletheG1phase-specificproteinCCNEisdownregulatedinadose-dependentmanner[1].XSJ151(88–600nM,48h)inducesapoptosisinAGSandMGC803cellsbysignificantlyupregulatingBADandBAXproteinsanddownregulatingBcl-2protein[1].XSJ151(88-600nM,48h)significantlyincreasesthenumberofγ-H2AXintranuclearspotsinAGSandMGC803cells,indicatingDNAdouble-strandbreaksandsignificantlyincreasedγ-H2AXproteinlevels[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEXSJ151(150-200μM,30min)effectivelyinhibitsTopoI-catalyzedDNArelaxation[1].XSJ151(44-600μM,48h)significantlydownregulatesTopoIproteininAGSandMGC803cells[1].CellCycleAnalysis[1]CellLine:AGScells,MGC803cellsConcentration:2.5nM,5nM,10nMIncubationTime:24hResult:InAGScells,theproportionofcellsinG2/Mphaseincreasedfrom14.96%to65.45%.InMGC803cells,itincreasedfrom16.74%to71.65%.REFERENCES[1].SiZ,etal.Camptothecin20(S)-sulfonylamidinederivativeinhibitsgastriccancercellproliferationbytargetingtopoisomeraseItotriggertheDNAdamage-apoptosiscascade.BioorgChem.2025Nov;166:109171.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplica