U0126isanon-ATPcompetitiveMEKinhibitor,withIC₅₀of70nMand60nMforMEK1andMEK2,respectively.

IC50:70/60nM(MEK1/2)^[1]

TreatmentwithU0126efficientlyreducesProgenyvirustitersofalltestedstrainsinA549cells.WhilenMconcentrationsofU0126areefficienttoreduceH1N1vandH5N1(MB1),μMconcentrationsofU0126arerequiredtoreducethevirustiterofH5N1(GSB)andH7N7.TheEC₅₀valuesforU0126againstH1N1vare1.2±0.4μMinA549cellsand74.7±1.0μMinMDCKIIcells^[2].Rathepatocarcinomacells(FAO)stimulatedbyfetalcalfserum(FCS)exhibitsasignificantproportioninSphase(32.62%)whereasU0126stronglydecreasestheproportionofcellsinSphase(9.92%)andincreasestheproportionofcellsinG₀-G₁phaseandtoalesserextentinG₂/M^[3].

MicearetreateddailywithU0126(i.p.,10.5mg/kg).Incontrolexperiment,tumorsizesareconstantorslightlyincreasealloverthekinetic.Attheopposite,inallU0126experiments,engraftmentandearlytumorgrowtharesignificantlydecreased.FurThermore,a60-70%reductioninthevolumeoftumorstreatedwithU0126isobtained9daysafterinjectionandthereafter^[3].Ratsaresubjectedto120?minutestransientmiddlecerebralarteryocclusion(tMCAO)andthereaftertreatedwiththeU0126(i.p.,30mg/kg)at0and24hoursofreperfusion.AftertreatmentwithU0126,thevasoconstrictiontoS6cismarkedlyreduced^[4].

• [1].DunciaJV,etal.MEKinhibitors:thechemistryandBIOLOGicalactivityofU0126,itsanalogs,andcyclizationproducts.BioorgMedChemLett.1998,8(20),2839-2844.

  [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.

U0126isdissolvedinDMSO(10mM)andstored,andthendilutedwithappropriatemedia(DMSO1%)beforeuse^[2].

A549andMDCKIIcellsareseededin96-wellcultureplatesatadensityof8×10⁴cellsperwellinminimalessentialmedium(MEM)containing10%heat-inactivatedfetalcalfserum(FCS),100U/mLPenicillin,100mg/mLStreptomycin.Cellsareincubatedat37°Cwith5%CO₂overnight.Thereafter,cellsarewashedtwicewithPBS.MEMcontainingdifferentconcentrationsofU0126(0.001-1000μM)isaddedtothecells.AfteradditionofU0126,cellsareincubatedfurtherfor48hat37°Cand5%CO₂.Then,cellsarefixedbyincubationfor30minat4°Cwith100μL4%paraformaldehyde(PFA).Adding100μLcrystalvioletfor30minatroomtemperaturestainedviablecells.Afterstaining,platesarewashedanddried.Fortheextractionofcrystalvioletfromviablecells100μLof100%methanolisaddedtoeachwell.Afterincubationfor30minatroomtemperature,theextinctionismeasuredwithanenzyme-linkedimmunosorbentassay(ELISA)readeratOD=490nm.ThepercentageofcellviABIlityaftertreatmentwiththeantiviralcompoundiscalculated^[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

U0126isdissolvedinDMSO.

Mice^[3]
Athymicfemalenudemice(SWISS,nu/nu)areused.Priortoinjection,FIcellsarelabeledwithastablefluorescentdyemolecule,DiAat10μg/mLfor5hat37°C.AfterwashingtoremovefreeDiA,cellsaretrypsinizedforinoculation(U0126experiments)ortransfection(RNAiexperiments).Biliaryepithelialcellsareinjectedsubcutaneously,attheindicatedtimes,intothetibiaofnudemice.Inthechemicalexperiments,3hafterinoculation,micearetreatedwithU0126(10.5mg/kg)dailybyintraperitonealinjection.Thelengthandwidthofeachtumoraremeasuredeverydaybyusingacaliper.Thefollowingformulaisusedtocalculatetumorvolumes=width²×length/2.Micearekilledattheendofexperiment.Tumorsareimmediatelyfrozeninliquidnitrogen.
Rat^[4]
Twelve-week-oldfemaleWistarrats(250to265g)areusedU0126(30mg/kgintraperitoneally)isinjectedat0and24hoursofreperfusionaftertMCAObasedonthepreviousevaluationofthedruginmalerats.AnimalsinstudyIIareadministeredU0126orvehicleandarekilled14daysaftertMCAO.Experimentalgroupassignmentsarerandomizedandblindedtothesurgicalexperimenter.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

• [1].DunciaJV,etal.MEKinhibitors:thechemistryandbiologicalactivityofU0126,itsanalogs,andcyclizationproducts.BioorgMedChemLett.1998,8(20),2839-2844.

  [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.

426.56

C₂₀H₂₂N₆OS₂

1173097-76-1

RoomtemperatureincontinentalUS;mayvaryelsewhere

DMSO:≥49mg/mL

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:98.03%

SelectBatch:HY-12031-19826HY-12031-11718

DataSheet(124KB)SDS(120KB)

COA(94KB)HNMR(207KB)LCMS(237KB)

HandlingInstructions(1252KB)

• [1].DunciaJV,etal.MEKinhibitors:thechemistryandbiologicalactivityofU0126,itsanalogs,andcyclizationproducts.BioorgMedChemLett.1998,8(20),2839-2844.

  [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.

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Medchemexpress/Plerixafor octahydrochloride(Synonyms: AMD3100 octahydrochloride; JM3100 octahydrochloride; SID791 octahydroch

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