Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETubulinpolymerization-IN-13Cat.No.:HY-146209CASNo.:2426665-56-5分?式:C??H??NO?分?量:371.38作?靶點:Microtubule/Tubulin;Apoptosis作?通路:CellCycle/DNADamage;Cytoskeleton;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Tubulinpolymerization-IN-13(Compound4f)?種微管蛋?聚集抑制劑(IC50=0.37μM)。Tubulinpolymerization-IN-13表現(xiàn)出對癌細胞的抗增殖活性，可誘導(dǎo)細胞凋亡，具有潛在的抗?管活性。IC50&TargetIC50:0.37μM(tubulinpolymerization)[1]體外研究Tubulinpolymerization-IN-13(0.005-2.8nM)treatmentinhibitstumorcellproliferation[1].Tubulinpolymerization-IN-13(8.7-10μM)isnon-toxicinnon-tumorcells[1].Tubulinpolymerization-IN-13(1-50nM;24h)treatmentinducescellcyclearrestinG2/M[1].Tubulinpolymerization-IN-13(10nM;24and48h)treatmentinducescellapoptosis[1].Tubulinpolymerization-IN-13(10-100nM;24h)treatmentinducesalterationofthemicrotubulenetwork[1].CellProliferationAssay[1]CellLine:HeLa,HT-29,Daoy,HL-60,SEM,andJurkatcellsConcentration:0.005-2.8nMIncubationTime:Result:ShowedIC50sof2.8nM,2.1nM,0.005nM,2.7nM,0.31nM,and0.28nMforHeLa,HT-29,Daoy,HL-60,SEM,andJurkatcells,respectively.CellCytotoxicityAssay[1]CellLine:Peripheralbloodlymphocytes(PBL)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:8.7-10μMIncubationTime:Result:ShowedaGI50of8.7μMinquiescentlymphocytes.CellCycleAnalysis[1]CellLine:HeLacellsConcentration:1,5,10,and50nMIncubationTime:24hoursResult:InducedaG2/Marrestat10nM,increasedG2/McellsaccompaniedbyastrongreductionofcellsintheG1phase.ApoptosisAnalysis[1]CellLine:HeLacellsConcentration:10nMIncubationTime:24and48hoursResult:Inducedcaspase-9activation,PARPcleavage,Bcl-2phosphorylationandMcl-1downregulation.Immunofluorescence[1]CellLine:HeLacellsConcentration:10,50,and100nMIncubationTime:24hoursResult:Showedthedisorganizationofmicrotubulesat10nM,andmuchmoreevidentat50and100nM.體內(nèi)研究Tubulinpolymerization-IN-13(intraperitonealinjection;15or5mg/kg;onceeveryotherday;4times)reducestumorgrowthinadose-dependentmannerinanorthotopicmurinetumormodel[1].AnimalModel:Seven-week-oldC57BL/6femalemiceorthotopicallyinjectedintothemammaryfatpadwithE0771mammarycarcinomacells[1]Dosage:15or5mg/kgAdministration:Intraperitonealinjection;15or5mg/kg;onceeveryotherday;4times2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Reducedtumormassby45.7%and16.9%at15and5mg/kg,respectively.Showednosignoftoxicityandnodecreasementinanimalbodyweight.REFERENCES[1].PaolaOliva,etal.Design,synthesis,invitroandinvivobiologicalevaluationof2-amino-3-aroylbenzo[b]furanderivativesashighlypotenttubulinpolymerizationinhibitors.EurJMedChem.2020Aug15;200:112448.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo