Isoangustone-A-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEIsoangustoneACat.No.:HY-N4006CASNo.:129280-34-8分子式:C??H??O?分子量:422.47作用靶點(diǎn):Apoptosis;Autophagy作用通路:Apoptosis;Autophagy儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性IsoangustoneA是一種抗癌和抗炎劑。IsoangustoneA誘導(dǎo)癌細(xì)胞凋亡(apoptosis)和自噬(autophagic)[1][2][3]。IC50&TargetApoptosis,Autophagy[2]體外研究IsoangustoneA(10and20μM;48and72h)suppressesproliferationandinducesG1phasecellcyclearrestinSK-MEL-28cells[1].IsoangustoneA(10and20μM;48h)decreasestheabundanceofG1phase-relatedproteinsmediatedthroughtheAkt/GSK3βandMKK4/MKK7/JNKssignalingpathways[1].IsoangustoneAsuppressesPI3-K,MKK4,andMKK7kinaseactivitiesbydirectlybindinginanATP-competitivemanner[1].IsoangustoneA(20μM;0.5-4h)inducesautophagyincolorectalcancercellsbyactivatingAMPKsignaling[2].IsoangustoneA(1-20μM;0-100min)inhibitsmitochondrialrespiration[2].IsoangustoneA(15μM;6h)inducesSW480cellsapoptosis[2].IsoangustoneA(1-20μΜ;3days)suppressesmesangialfibrosisandinflammationinhumanrenalmesangialcells[3].CellProliferationAssay[1]CellLine:SK-MEL-28Concentration:10and20μM1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEIncubationTime:48and72hResult:Inhibitedproliferationinadose-andtime-dependentmanner.CellCycleAnalysis[1]CellLine:SK-MEL-28Concentration:10and20μMIncubationTime:48hResult:CausedcellcyclearrestatG1phase.WesternBlotAnalysis[1]CellLine:SK-MEL-28Concentration:10and20μMIncubationTime:48hResult:InhibitedtheexpressionofcyclinD1andcyclinE.SuppressedphosphorylationofRbinadose-dependentmanner.InhibitedthephosphorylationofAkt(Ser473,Thr308)andGSK3β(Ser9).SuppressedthephosphorylationofJNK1/2,buthadnoeffectonERK1/2orp38.CellAutophagyAssay[2]CellLine:SW480cellsConcentration:20μMIncubationTime:0.5,2and4hResult:Deformedmitochondria,nondegradablecellulardebriswereallobservabletogetherwithautophagicvacuolesincellsafter4h.ApoptosisAnalysis[2]CellLine:SW480cellsConcentration:15μMIncubationTime:6hResult:InducedelevationofapoptoticAnnexinV+/PI-andAnnexinV+/PI+cellpopulations.體內(nèi)研究IsoangustoneA(2or10mg/kg;i.p.;dailyfor35days)significantlydecreasestumorgrowth,volume,and2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEweightofSK-MEL-28xenograftsinmice[1].AnimalModel:MaleBalb/cnu/numice,SK-MEL-28xenograftmodel[1]Dosage:2or10mg/kgAdministration:Intraperitonealinjection,dailyfor35daysResult:Significantlysuppressedtumorweightcomparedtothecontrolgroup.Markedlyinhibitedtheexpressionofproliferatingcellnuclearantigen(PCNA).DecreasedphosphorylationlevelsofAkt.REFERENCESSongNR,etal.IsoangustoneA,anovellicoricecompound,inhibitscellproliferationbytargetingPI3K,MKK4,andMKK7inhumanmelanoma.CancerPrevRes(Phila).2013Dec;6(12):1293-303.TangS,etal.IsoangustoneAinducesautophagiccelldeathincolorectalcancercellsbyactivatingAMPKsignaling.Fitoterapia.2021Jul;152:104935.LiJ,etal.IsoangustoneAsuppressesmesangialfibrosisandinflammationinhumanrenalmesangialcells.ExpBiolMed(Maywood).2011Apr1;236(4):435-44.McePdfHeightCaution:Producthasnotbeen