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    U0126-EtOH
    U0126-EtOH

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0447
    CAS #: 1173097-76-1 Purity ≥98%

    Description: U0126-EtOH is a novel, selective and non-ATP competitive MEK1/2  inhibitor with potential anticviral activity. It inhibits MEK1/2 with IC50s of 0.07 μM/0.06 μM in cell-free assays. 

    References: Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44; Behav Brain Res. 2012 Jun 15;232(1):165-73.

    Related CAS: 109511-58-2 (U0126 free);  1173097-76-1 (EtOH)

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    • 香港大学
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    Molecular Weight (MW)426.56
    FormulaC18H16N6S2.C2H6O
    CAS No.1173097-76-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 85 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)10% DMSO+50% PEG 300+ddH2O: 28mg/mL
    Synonyms

    U0126, U-0126-EtOH; U0126 EtOH, U 0126, U-0126; U0126-EtOH, U 0126-EtOH, U 0126 EtOH, U-0126 EtOH

    Chemical Name: (2Z,3Z)-2,3-bis(amino((2-aminophenyl)thio)methylene)succinonitrile compound with ethanol (1:1)

    InChi Key: CFQULUVMLGZVAF-OYJDLGDISA-N

    InChi Code: InChI=1S/C18H16N6S2.C2H6O/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22;1-2-3/h1-8H,21-24H2;3H,2H2,1H3/b17-11+,18-12+;

    SMILES Code: CCO.C1=CC=C(C(=C1)N)SC(=C(C#N)C(=C(N)SC2=CC=CC=C2N)C#N)N 


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    In Vitro

    In vitro activity: U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. U0126-EtOH inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs without effect on IL-2-induced proliferation by down-regulating IL-2 mRNA levels. A recent study shows that U0126-EtOH antagonizes resveratrol-induced apoptosis in castration-resistant human prostate cancer C4-2 cells, inhibits mitochondrial function and shifts cells to aerobic glycolysis independently of MEK.


    Kinase Assay: The amount of immunoprecipitated wild type MEK used in these assays is adjusted to give a similar amount of activity units as obtained with 10 nM recombinant MEK. Reaction velocities are measured using a 96-well nitrocellulose filter apparatus as described below. Unless otherwise noted, reactions are carried out at an enzyme concentration of 10 nM, in 20 mM Hepes, 10 mM MgCl2, 5 mM β-mercaptoethanol, 0.1 mg/mL BSA, pH 7.4, at room temperature. Reactions are initiated by the addition of [γ-33P]ATP into the premixed MEK/ERK/inhibitor reaction mixture, and an aliquot of 100 μL is taken every 6 minutes and transferred to the 96-well nitrocellulose membrane plate which has 50 mM EDTA to stop the reaction. The membrane plate is drawn and washed 4 times with buffer under vacuum. Wells are then filled with 30 μL of Microscint-20 scintillation fluid, and the radioactivity of 33P-phosphorylated ERK is counted with a Top Count scintillation counter. Velocities are obtained from the slopes of radioactivity versus time plots. Concentrations of ERK and ATP are 400 nM and 40 μM, respectively, unless otherwise indicated. For all of the in vitro enzyme assays, the percent inhibition is calculated 100 (1 −Vi/Vo) where Vi and Vo are the initial reaction velocities in the presence and absence of inhibitor, respectively. The data are then plotted as percent inhibition as a function of inhibitor concentration and fit, by nonlinear least squares regression, to the standard equation for a Langmuir isotherm to determine the IC50. As reported, enzyme concentrations are based upon molecular weights and mass of protein used in the final assay volume and not on active site titration. Thus, the actual enzyme active site concentration may differ from that reported.


    Cell Assay:  A.E7 or Th17 cells are incubated with mitomycin C-treated B10.BR or BALB/c splenocytes plus varying concentrations of pigeon cytochrome c or PR8 Ag, or with 5 U/mL human rIL-2. In addition, some assays contains U0126 or an inactive analogue, U0124, to determine direct effects of MEK inhibition on T cell proliferation. Two days after culture initiation, each well is pulsed with 1 µCi of [3H]TdR and harvested the following day. The incorporation of [3H]TdR into DNA is quantitated on a Packard Matrix 96 direct beta counter without the use of liquid scintillation mixtures.

    In VivoU0126-EtOH, as the inhibitor of intracellular Raf/MEK/ERK signaling pathway, demonstrates antiviral activity by suppressing propagation of the 2009 pandemic IV H1N1 variant and highly pathogenic avian influenza viruses (HPAIV) in vivo in the mouse lung by inhibiting. U0126-EtOH shows the potential neuroprotective effect and improving spatial learning in Morris water maze (MWM) by activating peroxisome proliferator-activated receptor gamma coactivator-1a, nuclear respiratory factor 1, and mitochondrial transcription factor A in Aβ-injected rats.
    Animal modelFemale C57Bl/6 mice infected by Mouse-adapted highly pathogenic avian influenza A/FPV/Bratislava/79 (H7N7; FPV) virus and swine origin human influenza A virus (SOIV) A/Regensburg/D6/2009 (H1N1v; RB1).
    Formulation & DosageDissolved in 10% DMSO, 30% of Cremophor EL and 60% PBS; ≤10 mM;   Administered via aerosol.
    References

    Bioorg Med Chem Lett. 1998 Oct 20;8(20):2839-44; Behav Brain Res. 2012 Jun 15;232(1):165-73.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    U0126


    Increased endothelin type B (ETB) receptor-mediated vasoconstriction and p-ERK1/2 expression in female rat MCAs.  2015 Mar;35(3):454-60.

     U0126


    Ischemia-induced increase in smooth muscle endothelin type B (ETB) receptor and p-ERK1/2 expression after transient middle cerebral artery occlusion (tMCAO) is prevented by U0126 treatment. (A) Representative images of ETB receptor and (B) p-ERK1/2 expression at 48 hours of reperfusion after tMCAO in the occluded and non-occluded middle cerebral artery (MCA) in untreated, vehicle, and U0126 animals. Scale bar: 50 μm. (C) Quantification (mean fluorescence intensity in the smooth muscle cell layer of the occluded MCA normalized to the non-occluded MCA) of ETB receptor and (D) p-ERK1/2 expression.  2015 Mar;35(3):454-60.

     U0126


    MEK1/2 inhibition results in improved neurologic function after transient middle cerebral artery occlusion (tMCAO). (A) Infarct volume from untreated (n=7), vehicle (n=4), and U0126-treated (n=9) rats at 48 hours of reperfusion after tMCAO. (B) Representative NeuN immunostaining of brain slices from Bregma −2.2 to +3.8 is shown (1 mm interval). The border between nonlesioned (NeuN positive) and lesioned areas is depicted in the untreated group. (C) Recovery of sensorimotor function up to 14 days after tMCAO with the 28-point neuroscore. (D) Gross neurologic function graded in six levels from 0—no visible defects to 5—death.   2015 Mar;35(3):454-60.

    U0126

     

    U0126

     

    U0126

    Experimental design.  2015 Mar;35(3):454-60.


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