TMLB-C16-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETMLB-C16Cat.No.:HY-177796CASNo.:2923531-50-2分⼦式:C₂₃H₂₀ClN₃O₅分⼦量:453.88作⽤靶点:Apoptosis;CDK;Caspase;PARP作⽤通路:Apoptosis;CellCycle/DNADamage;Epigenetics储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性TMLB-C16⼀种强效且⼝服有效的B3GAT3抑制剂，其KD值为3.962μM。TMLB-C16可抑制MHCC-97H(IC50=6.53μM)和HCCLM3(IC50=6.22μM)细胞的增殖和迁移，并诱导细胞周期阻滞和凋亡(apoptosis)。TMLB-C16在MHCC-97H和HCCLM3异种移植瘤⼩⿏模型中均能抑制肿瘤⽣长，且未观察到明显的毒性。TMLB-C16可⽤于肝细胞癌的研究[1]。体外研究TMLB-C16(72h)demonstratesbroadantitumoractivitiesin13B3GAT3highexpressedcancercelllines(suchasNCI-H460,NCI-H1650,andCalu3cells)inaB3GAT3-dependentmanner,withIC50valuesbelow20μM[1].TMLB-C16(0-10μM,14days)preventscolonyformationinadose-dependentmannerinMHCC-97HandHCCLM3cells[1].TMLB-C16(0-10μM,24h)inhibitscellmigrationandinhibitscelldivisioninMHCC-97HandHCCLM3cells[1].TMLB-C16(0-10μM,48h)inducesG0/G1-phasecellcyclearrestandapoptosisinMHCC-97HandHCCLM3cellsinadose-dependentmanner,accompaniedbyenhancedp21,p53,andretinoblastoma-associatedprotein(Rb)levelsanddecreasedCDK6,cyclinE1,andphosphorylated-Rb(p-Rb)levels[1].CellProliferationAssay[1]CellLine:MHCC-97HandHCCLM3cellsConcentration:0,5,and10μMIncubationTime:14days1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Preventedcolonyformationinadose-dependentmanner.CellMigrationAssay[1]CellLine:MHCC-97HandHCCLM3cellsConcentration:0,5,and10μMIncubationTime:24hResult:SuppressedthewoundhealingofMHCC-97HandHCCLM3cellsfromabout22.22%to0.86%and15.71%to1.90%,respectively.CellCycleAnalysis[1]CellLine:MHCC-97HandHCCLM3cellsConcentration:0,5,and10μMIncubationTime:24hResult:RemarkablyrepressedthepercentageofS-phaseinMHCC-97HandHCCLM3cellsattheconcentrationof10and5μM,respectively,byaccumulatingcellsintheG0/G1-phase.WesternBlotAnalysis[1]CellLine:MHCC-97HandHCCLM3cellsConcentration:0,5,and10μMIncubationTime:48hResult:InducedexpressionoftheepithelialsurfacemarkerE-cadherinaswellaslossofthemesenchymalmarkerssuchasN-cadherin,vimentin,matrixmetalloproteinase-2(MMP-2),MMP-9,andzincfingerE-box-bindinghomeobox1(ZEB1).Significantlyenhancedexpressionofp21,p53,andRb,anddecreasedCDK6,cyclinE1,andp-Rbinadose-dependentmanner.Remarkablyenhancedtheexpressionlevelsofactivec-PARPandc-caspase-3inMHCC-97HandHCCLM3cells.ApoptosisAnalysis[1]CellLine:MHCC-97HandHCCLM3cellsConcentration:0,5,and10μMIncubationTime:48h2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Inducedapoptosisatbothtestedconcentrations.IncreasedtheearlyandlateapoptoticratesinMHCC-97Hat5μMby8.09%and6.21%,respectively.IncreasedtheearlyandlateapoptoticratesinMHCC-97Hat10μMby29.93%and15.77%,respectively.体内研究TMLB-C16(5,10and20mg/kg,i.g.,dailyfromday7today31)inhibitstumorgrowthinbothMHCC-97HandHCCLM3xenografttumormousemodels[1].AnimalModel:MaleBALB/cnudemice(6-8weeks)subcutaneouslyinjectedwithMHCC-97HandHCCLM3cells[1]Dosage:5,10and20mg/kgAdministration:i.g.,dailyfromday7today31Result:Exhibitedadose-dependenttumorinhibitioneffectinMHCC-97Hxenograftmodelwith70%and73.49%tumorgrowthinhibitionatdosesof10and20mg/kg,respectively.Exhibitedatumorgrowthinhibitionrateofapproximately59%atthedoseof10mg/kginHCCLM3xenograftmodel.REFERENCES[1].YinH,etal.DiscoveryofNovel2-OxoacetamideDerivativesasB3GAT3InhibitorsfortheTreatmentofHepatocellularCarcinoma.JMedChem.2024Jul11;67(13):10743-10773.McePdfHeightCautio