2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. MEK

MEK

Mitogen-activated protein kinase kinase; MAPKK; MAP2K

MEK

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MEK (Mitogen-activated protein kinase kinase, MAPKK) is a kinase enzyme which phosphorylates mitogen-activated protein kinases (MAPKs). The activated MAPK leads to the phosphorylation of downstream transcription factors that regulate various responses such as stress signaling, pathogen response, and hormone signaling.

In general, the MAPKKK phosphorylates a serine or threonine residue on a MAPKK, which sequentially activates a MAPK (ERK, p38 or JNK), the last protein in the cascade. Activation of the p38 MAPK occurs mainly through mitogen-activated protein kinase kinase 3 (MKK3) and MKK6 (sometimes MKK4). The JNK is regulated by two upstream MAP2Ks: MKK4 and MKK7. The highly homologous kinases, MEK1 and MEK2, act downstream of Ras and Raf to activate ERK mitogen-activated protein kinases.

MEK Isoform Specific Products:

MEK Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-164474
    DS03090629
    		Inhibitor
    DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy.
    DS03090629
  • HY-RS08041
    MAP2K5 Human Pre-designed siRNA Set A
    		Inhibitor

    MAP2K5 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K5 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MAP2K5 Human Pre-designed siRNA Set A
  • HY-B0185BR
    Lidocaine hydrochloride hydrate (Standard)
    		Inhibitor
    Lidocaine (hydrochloride hydrate) (Standard) is the analytical standard of Lidocaine (hydrochloride hydrate). This product is intended for research and analytical applications. Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine hydrochloride hydrate (Standard)
  • HY-137881
    MEK-IN-4
    		Inhibitor
    MEK-IN-4 is a MEK inhibitor. MEK-IN-4 can be used for the research of inflammatory disorders and cancers.
    MEK-IN-4
  • HY-19700R
    trans-Zeatin (Standard)
    		Inhibitor
    trans-Zeatin (Standard) is the analytical standard of trans-Zeatin. This product is intended for research and analytical applications. trans-Zeatin is a plant cytokinin, which plays an important role in cell growth, differentiation, and division; trans-Zeatin also inhibits UV-induced MEK/ERK activation.
    trans-Zeatin (Standard)
  • HY-10999S2
    Trametinib-13C,d3
    		Inhibitor
    Trametinib-13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
    Trametinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-RS08034
    Map2k1 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Map2k1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map2k1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k1 Mouse Pre-designed siRNA Set A
  • HY-P10832
    ATWLPPRAANLLMAAS
    		Inhibitor
    ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent anti-tumor effects. ATWLPPRAANLLMAAS can inhibit the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induce apoptosis..
    ATWLPPRAANLLMAAS
  • HY-E70745
    MEK1 P124L Recombinant Human Active Protein Kinase
    MEK1 is the MAP/ERK kinase. The MEK1 kinase directly phosphorylates ERK2, after the activation loop of MEK1 is itself phosphorylated by Raf. MEK1 P124L is a mutant of MEK1. MEK1 P124L Recombinant Human Active Protein Kinase is a recombinant MEK1 P124L protein that can be used to study MEK1 P124L-related functions.
    MEK1 P124L Recombinant Human Active Protein Kinase
  • HY-50295A
    CI-1040 hydrochloride
    		Inhibitor
    CI-1040 (PD 184352) hydrochloride is an orally active, highly specific inhibitor of MEK, with an IC50 of 17 nM for MEK1.
    CI-1040 hydrochloride
  • HY-153864
    PROTAC MEK1 Degrader-1
    		Inhibitor
    PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells.
    PROTAC MEK1 Degrader-1
  • HY-153445A
    Polfurmetinib hydrate
    		Inhibitor
    Polfurmetinib (MEK-IN-6) hydrate (compound 69) is a MEK inhibitor. Polfurmetinib hydrate has an IC50 of 2 nM for A375 cells.
    Polfurmetinib hydrate
  • HY-13064R
    Cobimetinib (Standard)
    		Inhibitor
    Cobimetinib (Standard) is the analytical standard of Cobimetinib. This product is intended for research and analytical applications. Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
    Cobimetinib (Standard)
  • HY-50706R
    Selumetinib (Standard)
    		Inhibitor
    Selumetinib (Standard) is the analytical standard of Selumetinib. This product is intended for research and analytical applications. Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
    Selumetinib (Standard)
  • HY-164529
    SJ-C1044
    SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer.
    SJ-C1044
  • HY-P0119S
    Lixisenatide (Leu-13C6,15N) TFA
    		Inhibitor
    Lixisenatide (Leu-13C6,15N) TFA is the 13C- and 15N-labeled Lixisenatide (HY-P0119). Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of pro-inflammatory cytokines, and suppresses of the Akt-MEK1/2 signaling pathway. Lixisenatide can inhibit oxidative stress, mitochondrial dysfunction and apoptosis. Lixisenatide can be used for the researches of inflammation, metabolic disease, neurological disease and cardiovascular disease, such as rheumatoid arthritis, diabetes, Alzheimer's disease and atherosclerosis.
    Lixisenatide (Leu-<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N) TFA
  • HY-N6670R
    Cefotetan (Standard)
    		Activator
    Cefotetan (Standard) is the analytical standard of Cefotetan. This product is intended for research and analytical applications. Cefotetan is a semisynthetic cephamycin antibiotic that exerts its bactericidal effects by inhibition of cell-wall synthesis.
    Cefotetan (Standard)
  • HY-B0185S
    N-Oxide Lidocaine-d10
    		Inhibitor
    N-Oxide Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia.
    N-Oxide Lidocaine-d<sub>10</sub>
  • HY-101481R
    Flurbiprofen axetil (Standard)
    		Inhibitor
    Flurbiprofen axetil (Standard) is the analytical standard of Flurbiprofen axetil. This product is intended for research and analytical applications. Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway.
    Flurbiprofen axetil (Standard)
  • HY-15202S3
    Binimetinib-d4
    		Inhibitor
    Binimetinib-d4 (MEK162-d4) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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