MEK1 (MAPK/ERK kinase 1), also referred to as dual specificity mitogen-activated protein kinase kinase 1 (MAP2K1, MAPKK1) and ERK activator kinase 1 (ERK kinase 1), is a widely expressed cytoplasmic kinase from the protein kinase MAP kinase family. MEK1 and MEK2 are dual specificity enzymes that can phosphorylate threonine and tyrosine residues in their substrates. Although they are 86% identical in their catalytic domain, there is evidence that they may be regulated differentially. MEK1 contains an N-terminus with an inhibitory segment, a kinase domain with an ATP-binding site and a unique inhibitor binding pocket adjacent, and a C-terminal region. MEK1 is activated through its phosphorylation by upstream kinases such as RAF kinases, which leads to conformational changes in the kinase that allow it to phosphorylate ERK1/2 with high substrate specificity. As a critical component of the MAP kinase signal transduction pathway, MEK1 participates in signaling cascades that transmit a variety of extra- and intracellular signals to mediate diverse biological functions such as cell growth, adhesion, survival, and differentiation through regulation of transcription, metabolism, and cytoskeletal rearrangements. Constitutive activation of MEK1 was shown to stimulate cell proliferation directly and mitigate dependence on growth factors. Significant research has been performed to discover inhibitors of MEK1 as important research tools to facilitate understanding of ERK biology and also to target MEK1 for pharmacological intervention in cancer therapy and other diseases associated with MEK1 and MAP kinase pathway dysfunction.
Post-translational: Phosphorylation at Ser-218 and Ser-222 by MAP kinase kinase kinases (BRAF or MEKK1) positively regulates kinase activity (PubMed:29433126, PubMed:8131746). Also phosphorylated at Thr-292 by MAPK1/ERK2 and at Ser-298 by PAK (PubMed:16129686). MAPK1/ERK2 phosphorylation of Thr-292 occurs in response to cellular adhesion and leads to inhibition of Ser-298 phosphorylation by PAK (PubMed:16129686). Autophosphorylated at Ser-218 and Ser-222, autophosphosphorylation is promoted by NEK10 following UV irradiation (PubMed:20956560). (Microbial infection) Acetylation by Yersinia YopJ prevents phosphorylation and activation, thus blocking the MAPK signaling pathway.
生物活性
Immobilized Recombinant Human MEK1 Protein (rp230932) at 1.0 μg/mL can bind Recombinant MEK1 Antibody (Ab114854) with the EC50 of 21.4 ng/mL.
Store at -20℃ long term (6 months). Upon receipt, it is recommended to aliquot. Avoid freeze/thaw cycle.
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Recombinant Human MEK1 Protein (rp230932) - ELISA
Immobilized Recombinant Human MEK1 Protein (rp230932) at 1.0 μg/mL can bind Recombinant MEK1 Antibody (Ab114854) with the EC₅₀ of 21.4 ng/mL.
Recombinant Human MEK1 Protein (rp230932) - SDS-PAGE
2 μg/lane of Recombinant Human MEK1 Protein was resolved with SDS-PAGE under reducing (R) and non-reducing (N) conditions and visualized by Coomassie® Blue staining, showing the bands at 43.8 kDa under reducing conditions and 41.1-43.3 kDa under non-reducing conditions.
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