Tubulin-polymerization-IN-5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETubulinpolymerization-IN-5Cat.No.:HY-144299分⼦式:C₂₉H₃₉N₃O₈S₂分⼦量:621.77作⽤靶点:Microtubule/Tubulin;Apoptosis作⽤通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Tubulinpolymerization-IN-5(化合物20q)⼀种有效的具有潜在抗癌活性的微管蛋⽩抑制剂。Tubulinpolymerization-IN-5可以使ESCC细胞停滞在G2/M期，并导致细胞凋亡(apoptosis)[1]。IC50&TargetTubulin体外研究Tubulinpolymerization-IN-5(compound20q)(0-100nM,48h)exhibitspotentantiproliferativeactivityagainstKyse30,Kyse450,MGC-803,andHCT-116cells[1].Tubulinpolymerization-IN-5(0-60nM,7d)obviouslyinhibitsthecellularcolonyformationabilityoftheKyse30andKyse450cells[1].Tubulinpolymerization-IN-5(0-100nM,48h)inhibitsmicrotubuleassemblyanddisruptscytoskeleton[1].Tubulinpolymerization-IN-5(0-300nM,24h)causesasignificantweakeningoftheβ-tubulinadductbandinKyse30andKyse450cells,competitivelybindthecolchicinebindingsiteofβ-tubulin[1].Tubulinpolymerization-IN-5(0-100nM,48h)effectivelyarrestscellsattheG2/Mphase,andinducescellapoptosisinKyse30andKyse450cellsbyregulatingtheexpressionofrelatedproteins[1].Tubulinpolymerization-IN-5(0-100nM,48h)inducescellmitochondrialapoptosisinESCCcells,leadstoasignificantdepolarizationofmitochondriamembranepotentialinKyse30andKyse450cells[1].CellProliferationAssayCellLine:Kyse30,Kyse450,MGC-803,andHCT-116cells[1]Concentration:0,80,100nMIncubationTime:48h1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:ExhibitedpotentantiproliferativeactivityagainstKyse30,Kyse450,MGC-803,andHCT-116cells,withIC50valuesof0.069,0.078,0.084,and0.227μM,respectively.CellCycleAnalysisCellLine:Kyse30andKyse450cells[1]Concentration:0,80,100nMIncubationTime:48hResult:Effectivelyarrested2ESCCcellsattheG2/Mphase,significantlyincreasedofpercentagesofcellsattheG2/Mphasefrom19.38to76.9767inKyse30cells,and7.04333to80.8933inKyse450cells.ApoptosisAnalysisCellLine:Kyse30andKyse450cells[1]Concentration:0,80,100nMIncubationTime:48hResult:Dose-dependentlyinducedcellapoptosisinKyse30andKyse450cells,significantlyincreasedthepercentagesoftotalapoptoticcellsfrom8.1667%(0nM)to23.8%(80nM,Kyse30cells),34.0333%(80nM,Kyse450cells),38.633%(100nM,Kyse30cells),and57.3667%(100nM,Kyse450cells),respectively.WesternBlotAnalysisCellLine:Kyse30andKyse450cells[1]Concentration:0,80,100nMIncubationTime:48hResult:Dose-dependentlydown-regulatedtheexpressionoftheG2phaserelatedproteinsCDK1,CDC25candp-Wee1,up-regulatedtheleveloftheMphasemarkerproteinp-HistoneH3;up-regulatedtheactivityoftheexecutorsofapoptosiscaspase-3,up-regulatedthepro-apoptoticproteinsBaxandNoxa,anddown-regulatedtheanti-apoptoticproteinBcl-2,decreasedthelevelsofIAP(InhibitorofApoptosisProteins)familyproteinXIAP.REFERENCES[1].SunYX,etal.Design,synthesisandevaluationofnovelbis-substitutedaromaticamidedithiocarbamatederivativesascolchicinesite2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEtubulinpolymerizationinhibitorswithpotentanticanceractivities.EurJMedChem.2022;229:114069.McePdfHeightCaution:Producthasnotb