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Ion Channels >> Cell Signaling Tools >> Protein Kinases >> Inhibitors

U0126

A Specific MAPK Pathway Inhibitor
  • Bioassay tested
    Bioassay tested
  • Shipped at room temp.
    Shipped at room temp.
  • Cat #: U-400
  • Size: 1 mg, 5 x 1 mg, 5 mg, 10 x 0.1 mg
  • Source: Synthetic
  • MW: 380.5 Da.
General information
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 Mitogen-Activated Protein Kinase (MAPK) cascade by inhibiting its immediate upstream activators, Mitogen Activated Protein Kinase Kinase 1and 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 MEK (1,2). 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 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

Alomone Labs is pleased to offer U0126 (#U-400), a purified synthetic compound.
Our Bioassay
Specifications
References
 
Our bioassay
U0126 - 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.
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