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-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-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-B0185AR
    Lidocaine hydrochloride (Standard)
    		Inhibitor
    Lidocaine (hydrochloride) (Standard) is the analytical standard of Lidocaine (hydrochloride). This product is intended for research and analytical applications. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride 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 is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.
    Lidocaine hydrochloride (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
    Lixisenatide (Leu-13C6,15N) TFA is the 13C- and 15N-labeled Lixisenatide (HY-P0119). Lixisenatide is a GLP-1 receptor agonist. Lixisenatide inhibits the inflammatory response through down regulation of proinflammatory cytokines, and blocks of cellular signaling pathways. Lixisenatide decreases atheroma plaque size and instability in Apoe?/? Irs2+/? mice by reprogramming macrophages towards an M2 phenotype, which leads to reduced inflammation.
    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>
  • HY-12028R
    PD98059 (Standard)
    		Inhibitor
    PD98059 (Standard) is the analytical standard of PD98059. This product is intended for research and analytical applications. PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy.
    PD98059 (Standard)
  • HY-50706AR
    Selumetinib sulfate (Standard)
    		Inhibitor
    Selumetinib (sulfate) (Standard) is the analytical standard of Selumetinib (sulfate). 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 sulfate (Standard)
  • HY-128393S1
    Trilinolein-13C54
    		Inhibitor
    Trilinolein-13C54 is the 13C-labeled Trilinolein (HY-128393). Trilinolein is an orally active triglyceride that inhibits the PI3K/Akt, Ras/MEK/ERK signaling pathways, and MMP-2. Trilinolein can reduce oxidative stress, induce apoptosis, and inhibit cell migration. Trilinolein can be used in the research fields of cardiovascular disease, cerebrovascular disease (such as cerebral ischemia), and non-small cell lung cancer.
    Trilinolein-<sup>13</sup>C<sub>54</sub>
  • HY-50295R
    CI-1040 (Standard)
    		Inhibitor
    CI-1040 (Standard) is the analytical standard of CI-1040. This product is intended for research and analytical applications. CI-1040 (PD 184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
    CI-1040 (Standard)
  • HY-14719R
    RO4987655 (Standard)
    		Inhibitor
    RO4987655 (Standard) is the analytical standard of RO4987655. This product is intended for research and analytical applications. RO4987655 is an orally active and highly selective MEK inhibitor with an IC50 of 5.2 nM for inhibition of MEK1/MEK2.
    RO4987655 (Standard)
  • HY-126048
    JTP-70902
    		Inhibitor
    JTP-70902, a p15INK4b-inductive compound, is a MEK1/2 inhibitor. JTP-70902 exhibits potent antitumor effect.
    JTP-70902
  • HY-108635R
    C16-PAF (Standard)
    		Activator
    C16-PAF (Standard) is the analytical standard of C16-PAF. This product is intended for research and analytical applications. C16-PAF (PAF (C16)), a phospholipid mediator, is a platelet-activating factor and ligand for PAF G-protein-coupled receptor (PAFR). C16-PAF exhibits anti-apoptotic effect and inhibits caspase-dependent death by activating the PAFR. C16-PAF is a potent MAPK and MEK/ERK activator. C16-PAF induces increased vascular permeability.
    C16-PAF (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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