U0126-DataSheet-生命科学试剂-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEU0126Cat.No.:HY-12031ACASNo.:109511-58-2分⼦式:C₁₈H₁₆N₆S₂分⼦量:380.49作⽤靶点:MEK;Autophagy;Mitophagy;InfluenzaVirus作⽤通路:MAPK/ERKPathway;Autophagy;Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCOA.BIOLOGICALACTIVITY⽣物活性U0126⼀种有效，⾮ATP竞争性的，选择性的MEK1和MEK2抑制剂，IC50分别为72nM和58nM。U0126-EtOH⼀种⾃噬(autophagy)和线粒体⾃噬(mitophagy)抑制剂。IC50&TargetMEK2MEK160nM(IC50)70nM(IC50)体外研究TreatmentwithU0126efficientlyreducesprogenyvirustitersofalltestedstrainsinA549cells.WhilenMconcentrationsofU0126areefficienttoreduceH1N1vandH5N1(MB1),μMconcentrationsofU0126arerequiredtoreducethevirustiterofH5N1(GSB)andH7N7.TheEC50valuesforU0126-EtOHagainstH1N1vare1.2±0.4μMinA549cellsand74.7±1.0μMinMDCKIIcells[2].Rathepatocarcinomacells(FAO)stimulatedbyfetalcalfserum(FCS)exhibitsasignificantproportioninSphase(32.62%)whereasU0126stronglydecreasestheproportionofcellsinSphase(9.92%)andincreasestheproportionofcellsinG0-G1phaseandtoalesserextentinG2/M[3].CellViabilityAssay[2]CellLine:A549andMDCKIIcells.Concentration:0.001-1000μM.IncubationTime:48h.Result:TheEC50valuesforU0126againstH1N1vwere1.2±0.4μMinA549cellsand74.7±1.0μMinMDCKIIcells1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE体内研究MicearetreateddailywithU0126-EtOH(U0126;i.p.,10.5mg/kg).Incontrolexperiment,tumorsizesareconstantorslightlyincreasealloverthekinetic.Attheopposite,inallU0126-EtOHexperiments,engraftmentandearlytumorgrowtharesignificantlydecreased.Furthermore,a60-70%reductioninthevolumeoftumorstreatedwithU0126-EtOHisobtained9daysafterinjectionandthereafter[3].Ratsaresubjectedto120minutestransientmiddlecerebralarteryocclusion(tMCAO)andthereaftertreatedwiththeU0126-EtOH(U0126;i.p.,30mg/kg)at0and24hoursofreperfusion.AftertreatmentwithU0126-EtOH,thevasoconstrictiontoS6cismarkedlyreduced[4].AnimalModel:Athymicfemalenudemice(SWISS,nu/nu)[3].Dosage:10.5mg/kg.Administration:Intraperitonealinjectiondaily.Result:Inhibitedtumorgrowth.AnimalModel:Twelve-week-oldfemaleWistarrats(250to265g)[4].Dosage:30mg/kg.Administration:Intraperitoneally.Result:ThevasoconstrictiontoS6cismarkedlyreduced.•NatImmunol.2018Mar;19(3):233-245.•Blood.2018Jul12;132(2):210-222.•SignalTransductTargetTher.2020Aug26;5(1):153.•Biomaterials.2018Sep;178:95-108.•EMBOJ.2020Feb3;39(3):e102374.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FavataMF,etal.Identificationofanovelinhibitorofmitogen-activatedproteinkinasekinase.JBiolChem.1998Jul17;273(29):18623-32.[2].DroebnerK,etal.AntiviralactivityoftheMEK-inhibitorU0126againstpandemicH1N1vandhighlypathogenicavianinfluenzavirusinvitroandinvivo.AntiviralRes.2011,92(2),195-203.[3].BessardA,etal.RNAi-mediatedERK2knockdowninhibitsgrowthoftumorcellsinvitroandinvivo.Oncogene.2008Sep11;27(40):5315-25.[4].AhnstedtH,etal.U0126attenuatescerebralvasoconstrictionandimproveslong-termneurologicoutcomeafterstrokeinfemalerats.JCerebBloodFlowMetab.2015Mar;35(3):454-60.McePdfHeight2/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasno