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U0126

A Specific MAPK Pathway Inhibitor
Cat #: U-400
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 380.5
    Purity: >99%
    Effective concentration 0.1-100 µM.
    Structure
    Chemical name 1,4-Diamino-2,3-dicyano-1,4-bis[2- aminophenylthio]butadiene.
    Molecular formula C18H16N6S2.
    CAS No.: 109511-58-2.
    Activity U0126 specifically inhibits the kinase activity of mitogen activated protein kinase kinase (MAPKK, MEK1 and MEK2). It is less toxic than PD 980591,2.
    References-Activity
    1. Favata, M.F. et al. (1998) J. Biol. Chem273, 18623.
    2. Duncia, J.V. et al. (1998) Bioorg. Med. Chem. Lett. 8, 2839.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or six months at -20°C.
    Protect from light.
    Our bioassay
    • Alomone Labs U0126 inhibits P42/44 MAPK phosphorylation via MEK1/MEK2 in C6 glioma cells.
      Alomone Labs U0126 inhibits P42/44 MAPK phosphorylation via MEK1/MEK2 in C6 glioma cells.
      Cells were grown to 70% confluence and serum starved for 1.5 h. The cells were then incubated for 2 h with various concentrations of U0126 (#U-400) and stimulated with 7 ng/ml PDGF-AA. Cell proteins were resolved by SDS-PAGE and probed with anti-phospho-P42/44 MAPK (upper panel) and with anti-P42/44 MAPK (lower panel). The phosphorylation of P42/44 decreased in a dose-dependent manner.
    References - Scientific background
    1. Favata, M.F. et al. (1998) J. Biol. Chem273, 18623.
    2. Lockman, K. et al. (2004 ) J. Biol. Chem279, 42422.
    3. Cirillo, P. et al. (2004) Circulation 109, 2911.
    4. Duncia, J.V. et al. (1998) Bioorg Med Chem Lett8, 2839.
    5. Zhang, J. et al. (2004) Blood 104, 1679.
    6. Ninomiya, Y. et al. (2004) Cancer Res. 64, 2759.
    7. Sharma, PM. et al. (2005) Mol Endocrinol. 19, 421.
    8. Ichiki, T. et al. (2004) Biochem Biophys Res Commun323, 402.
    9. MacCormick, M. et al. (2005) Biochem J. 387, 155.
    10. Fukazawa, H. et al. (2000) Cancer Res60, 2104.
    Scientific background

    U0126 is a chemically synthesized organic compound that was initially recognized as a cellular AP-1 antagonist, and found to be a very selective and highly potent inhibitor of the Mitogen-Activated Protein Kinase (MAPK) cascade by inhibiting its immediate upstream activators, Mitogen-Activated Protein Kinase Kinase 1 and 2 (also known as MEK1 and MEK2, IC50: 70 and 60 nM respectively). U0126 inhibits both active and inactive MEK1,2, unlike PD098059 which only inhibits activation of inactive MEK1,2. Blockade of MEK activation would prevent downstream phosphorylation of a number of factors including p62TCF (Elk-1), an upstream inducer of c-Fos and c-Jun, components of the AP-1 complex.1-4

    Inhibition of the MEK/ERK pathway by U0126 also prevents all effects of oncogenic H-Ras and K-Ras, inhibits part of the effects triggered by growth factors and blocks the production of inflammatory cytokines and matrix metalloproteinases.5-11

    Last update: 16/08/2020

    U0126 (#U-400) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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    Scientific Background

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