8-Aminoadenosine-8-NH2-Ado-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemE8-AminoadenosineCat.No.:HY-125927CASNo.:3868-33-5Synonyms:8-NH2-Ado分⼦式:C₁₀H₁₄N₆O₄分⼦量:282.26作⽤靶点:DNA/RNASynthesis;Akt;mTOR;Autophagy;Apoptosis作⽤通路:CellCycle/DNADamage;PI3K/Akt/mTOR;Autophagy;Apoptosis储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.溶解性数据体外实验DMSO:83.33mg/mL(295.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5428mL17.7142mL35.4283mL5mM0.7086mL3.5428mL7.0857mL10mM0.3543mL1.7714mL3.5428mLBIOLOGICALACTIVITY⽣物活性8-Aminoadenosine(8-NH2-Ado)⼀种RNA导向的核苷类似物，可降低细胞ATP⽔平并抑制mRNA合成。8-Aminoadenosine阻断Akt/mTOR信号，并诱导p53⾮依赖性的⾃噬和细胞凋亡。8-Aminoadenosine具有抗肿瘤活性。IC50&TargetAktmTOR体外研究8-Aminoadenosine(8-NH2-Ado;0.1-10μM;for48h)hasIC50sof1.5μMand8.88μMinMM.1SandU266cells,respectively[1].1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE8-Aminoadenosine(10μM;for24h)inducessignificantapoptoticdeathofMCF-7cellsinp53-independentpathway.8-AminoadenosinecausesPARPcleavageinMCF-7cells[2].8-Aminoadenosine(3μM;0.5-4h)inducesautophagyintheMM.1Scellline[1].8-Aminoadenosine(3μM;2-16h)causesagreaterdropinATPlevelsintheMM.1Scells[1].8-Aminoadenosine(3μM;5h)causesa50%reductioninglucoseconsumptioninMM.1Scells[1].8-Aminoadenosine(3μM;5h)indicatesatime-dependentdecreaseinGLUT1expressionat5h,whereasat24htherewasadown-regulationofbothtransporters(GLUT1andGLUT4)inMM.1Scells[1].8-Aminoadenosineinhibitscellproliferation,activatedcelldeath,anddoesnotactivatetranscriptionofthep53targetgenep21orincreaseproteinlevelsofeitherp53orp21[1].Thetoxiceffectsof8-Aminoadenosinerequireadenosinekinaseactivitytoconvert8-Aminoadenosineto8-NH2-ATPinadenosinekinase-deficientcells[1].CellViabilityAssay[1]CellLine:MM.1SandU266cellsConcentration:0.1,0.3,1,3,10μMIncubationTime:For48hoursResult:HadIC50sof1.5μMand8.88μMinMM.1SandU266cells,respectively.ApoptosisAnalysis[2]CellLine:MCF-7cellsConcentration:10μMIncubationTime:For24hoursResult:Inducedsignificantapoptoticdeath.Apoptosiswasnotinhibitedbyknockdownoffunctionalp53.ApoptosisAnalysis[1]CellLine:MM.1ScelllineConcentration:3μMIncubationTime:0.5,1,1.5,2,2.5,3,3.5,4hoursResult:InducedtheformationofLC3-IIprotein.CausedtheappearanceofapopulationwithahighAVOcontentwith1μMfor24hours.REFERENCES[1].MalaShanmugam,etal.Targetingglucoseconsumptionandautophagyinmyelomawiththenovelnucleosideanalogue8-aminoadenosine.JBiolChem.2009Sep25;284(39):26816-30.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[2].JenniferAnnFrey,etal.8-Amino-adenosineinhibitsmultiplemechanismsoftranscription.MolCancerTher.2010Jan;9(1):236-45.[3].AllaPolotskaia,etal.8-Amino-adenosineactivatesp53-independentcelldeathofmetastaticbreastcancers.MolCancerTher.2012Nov;11(11):2495-504.McePdfHeightCaution:Producthasnotbeenfullyvalidat