Topoisomerase-I-II-inhibitor-3-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETopoisomeraseI/IIinhibitor3Cat.No.:HY-146504分?式:C??H??N?O?分?量:404.46作?靶點:Topoisomerase;PI3K;Apoptosis;ROSKinase作?通路:CellCycle/DNADamage;PI3K/Akt/mTOR;Apoptosis;ProteinTyrosineKinase/RTK儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性TopoisomeraseI/IIinhibitor3(7)?種有效的拓撲異構(gòu)酶I(TopoI)和II(TopoII)雙抑制劑。TopoisomeraseI/IIinhibitor3通過抑制PI3K/Akt/mTOR信號通路抑制細胞增殖、侵襲和遷移，誘導細胞凋亡(apoptosis)。TopoisomeraseI/IIinhibitor3可?于肝癌的研究[1]。IC50&TargetTopoisomeraseITopoisomeraseIIPI3K體外研究TopoisomeraseI/IIinhibitor3(compound7)(0-100μM)caninsertintoDNAandchangethetopologyofDNA,causeDNAdamagetoacertainextent[1].TopoisomeraseI/IIinhibitor3(0-4μM,24h)inhibitsHCC(hepatocellularcarcinoma)cellsproliferationinadose-dependentmanner,inhibitsmigrationandinvasionofLM9andHuH7cellsbyinhibitingtheexpressionofMMP-9[1].TopoisomeraseI/IIinhibitor3(0-14μM,48h)significantlyinducestheapoptosisofLM9andHuH7cells,andinducesmitochondrialdysfunctionandROSburstinadose-dependentmanner[1].TopoisomeraseI/IIinhibitor3(0-7μM,48h)reducestheexpressionoftheinhibitoryfactorBcl-2andpromotestheexpressionofmitochondria-dependentapoptosis-relatedproteinssuchasBax,cytochromeC,cleaved-caspase-3andcleaved-caspase-9;inhibitsthephosphorylationofPI3K/Akt/mTORsignalingpathway[1].CellProliferationAssayCellLine:HCCcells(HuH7andLM9)[1]Concentration:0,0.5,1,2,and4μM1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:24hResult:InhibitedHCCcellsproliferationinadose-dependentmanner,withIC50valuesof2.10μM(LM9)and1.93μM(HuH7),respectively,anddose-dependentlyinhibitedtheformationofcellcolonies.ApoptosisAnalysisCellLine:LM9andHuH7cells[1]Concentration:0,1.8,3.5,7,and14μMIncubationTime:48hResult:SignificantlyinducedtheapoptosisofLM9andHuH7cellsinaconcentration-dependentmanner.WesternBlotAnalysisCellLine:LM9andHuH7cells[1]Concentration:0,1.8,3.5,and7μMIncubationTime:48hResult:ReducedtheexpressionoftheinhibitoryfactorBcl-2andpromotedtheexpressionofmitochondria-dependentapoptosis-relatedproteinssuchasBax,cytochromeC,cleaved-caspase-3andcleaved-caspase-9;inhibitedthephosphorylationofPI3K/Akt/mTORsignalingpathway.體內(nèi)研究TopoisomeraseI/IIinhibitor3(compound7)(maleKunmingmice,0-400mg/kg,IP,once)causesthemiceinthe400mg/kggroupdie,withtheLD50between250and400mg/kg[1].AnimalModel:MaleKunmingmice(19-22mg,8mice,4groups)[1]Dosage:200,250,400mg/kg(dissolvedin5%DMSOandcastoroil)Administration:IP,onceResult:Didnotcausethemiceinthe250mg/kgand200mg/kggroupsdieafter2weeksofadministration,andcausedthemiceinthe400mg/kggroupdie,withtheLD50between250and400mg/kg.REFERENCES[1].DengX,LuoT,ZhangX,etal.Design,synthesisandbiologicalevaluationof3-arylisoquinolinederivativesastopoisomeraseIandII2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEdualinhibitorsforthetherapyoflivercancer.EurJMedChem.2022;237:114376.McePdfHeightCaution:Producthasnotbeenfu