Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETubulininhibitor23Cat.No.:HY-144818CASNo.:170488-57-0分?式:C??H??NO?S分?量:477.53作?靶點:Apoptosis;Microtubule/Tubulin作?通路:Apoptosis;CellCycle/DNADamage;Cytoskeleton儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Tubulininhibitor23?種有效的Tubulin抑制劑，IC50為4.8μM。Tubulininhibitor23誘導(dǎo)細(xì)胞凋亡(apoptosis)。Tubulininhibitor23以劑量依賴性?式顯?抗?管?成活性。Tubulininhibitor23具有研究??病的潛?[1]。IC50&TargetIC50:4.8μM(Tubulin)[1]體外研究Tubulininhibitor23(compound29e)(0-100μM)inhibitstubulinpolymerisation(IC50=4.8μM)andanti-angiogenesis(IC50=3.4μM)inZebrafish[1].Tubulininhibitor23(0-200nM;48h)inducescellapoptosisinaconcentration-dependentmanner[1].Tubulininhibitor23(0-20μM;0-29min)bindstothecolchicinesiteoftubulinandinhibitthemicrotubulepolymerisation[1].Tubulininhibitor23(0.1,1,10μM;1h)showsanti-angiogenesisactivitywithlowtoxicity(IC50=58.6μM)inHumanumbilicalveinendothelialcells(HUVECs)[1].CellProliferationAssay[1]CellLine:MV4-11,HL60,K562,THP-1,CCRF-CEM,Jurkat,HuT78cellsConcentration:IncubationTime:72hResult:ShowedpotentgrowthinhibitoryactivitywithIC50sof0.25,0.18,0.09,0.37,0.84,1.22,0.26μMforMV4-11,HL60,K562,THP-1,CCRF-CEM,Jurkat,HuT78cells,respectively.1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEApoptosisAnalysis[1]CellLine:K562cellsConcentration:0,50,100,200nMIncubationTime:48hResult:Thepercentageofapoptoticcellsignificantlyincreasedfrom5.95%to45.81%.WesternBlotAnalysis[1]CellLine:K562cellsConcentration:0,50,100,200nMIncubationTime:48hResult:Increasedtheexpressionofcleavedcaspase-3andPARP.體內(nèi)研究Tubulininhibitor23(2,6μM;addintoembryowater)showsantiangiogenicactivityinadose-dependentmanner[1].Tubulininhibitor23(2,6μM;addintoembryowater)suppressestheproliferationandmetastasisofK562cellsinzebrafishxenograftsinadose-dependentmanner[1].AnimalModel:3hpfzebrafishembryos[1]Dosage:2.0,6.0μMAdministration:AddintoembryowaterResult:DecreasedthenumberandlengthofISVs(intersegmentalvessels)inadose-dependentinhibitionpattern.AnimalModel:Transgeniczebrafish(fil1:EGFP)(K562cellxenograft)[1]Dosage:2,6μMAdministration:AddintoembryowaterResult:Reducedintensitiesanddecreasedtumourarea.REFERENCES[1].YaoY,wtal.Angiogenesisandanti-leukaemiaactivityofnovelindolederivativesaspotentcolchicinebindingsiteinhibitors.JEnzymeInhibMedChem.2022Dec;37(1):652-665.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapp