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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/U0126(Synonyms: U0126-EtOH)/HY-12031/50mg
商品详细Medchemexpress/U0126(Synonyms: U0126-EtOH)/HY-12031/50mg
Medchemexpress/U0126(Synonyms: U0126-EtOH)/HY-12031/50mg
Medchemexpress/U0126(Synonyms: U0126-EtOH)/HY-12031/50mg
商品编号： HY-12031-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
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商品介绍
U0126isanon-ATPcompetitiveMEKinhibitor,withIC50of70nMand60nMforMEK1andMEK2,respectively.

CustomerValidation

  • •FrontImmunol.2017Oct10;8:1278.
  • •CancerLett.2017Feb16;393:22-32.
  • •JMolCellCardiol.2015Dec;89(PtB):268-79.
  • •FreeRADIcBiolMed.2017Jul9;112:49-59.
  • •Oncotarget.2017May16;8(20):33807-33826.
  • •FrontMolNeurosci.2017Mar13;10:51.
  • •OxidMedCellLongev.2017;2017:7426458.
  • •OxidMedCellLongev.2017;2017:6175841.
  • •CellSignal.2017Jan16;32:48-58. 
  • •CellSignal.2016Feb;28(2):81-93.
  • •ACSChemNeurosci.2015Jan21;6(1):130-7.
  • •CellCycle.2017Apr3;16(7):714-722.
  • •Peptides.2016Oct14;86:72-79.
  • •IntJMolMed.2017Jul;40(1):164-174.
  • •IntJClinExpPathol.2017;10(7):7466-7474
  • •EnvironSciPollutResInt.2017Jul10.
  • •ThirdMilitaryMedicalUniversity
Description

U0126isanon-ATPcompetitiveMEKinhibitor,withIC50of70nMand60nMforMEK1andMEK2,respectively.

IC50&Target

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

InVitro

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].

InVivo

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].

References

  • [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.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.3443mL11.7217mL23.4434mL
5mM0.4689mL2.3443mL4.6887mL
10mM0.2344mL1.1722mL2.3443mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[2]

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.

AnimalAdmiNISTration
[3][4]

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.

References

  • [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.

MolecularWeight

426.56

Formula

C₂₀H₂₂N₆OS₂

CASNo.

1173097-76-1

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥49mg/mL

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

Purity:98.03%