Tubulin-inhibitor-23-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETubulininhibitor23Cat.No.:HY-144818CASNo.:170488-57-0分⼦式:C₂₆H₂₃NO₆S分⼦量:477.53作⽤靶点:Apoptosis;Microtubule/Tubulin作⽤通路:Apoptosis;CellCycle/DNADamage;Cytoskeleton储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Tubulininhibitor23⼀种有效的Tubulin抑制剂，IC50为4.8µM。Tubulininhibitor23诱导细胞凋亡(apoptosis)。Tubulininhibitor23以剂量依赖性⽅式显⽰抗⾎管⽣成活性。Tubulininhibitor23具有研究⽩⾎病的潜⼒[1]。IC50&TargetIC50:4.8µM(Tubulin)[1]体外研究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—您⾝边的抑制剂⼤师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.体内研究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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapp