CustomerValidation
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| Description | U0126isanon-ATPcompetitiveMEKinhibitor,withIC50of70nMand60nMforMEK1andMEK2,respectively. |
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| 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 |
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| PreparingStockSolutions |
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent. | ||||||||||||||||
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| 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] | ||||||||||||||||
| References |
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| MolecularWeight | 426.56 | ||||||||||||
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| Formula | C₂₀H₂₂N₆OS₂ | ||||||||||||
| CASNo. | 1173097-76-1 | ||||||||||||
| Storage |
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| Shipping | RoomtemperatureincontinentalUS;mayvaryelsewhere | ||||||||||||
| Solvent&Solubility | DMSO:≥49mg/mL *"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation=""> Purity:98.03% |
