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-E70842
    MAP2K1 L115P Recombinant Human Active Protein Kinase
    MAP2K1 (also known as MEK1) is downstream of the RAF family and activation results in ERK1/2 activation. Activating mutations in MAP2K1 have been reported almost exclusively in exons 1 and 2 in both hematologic malignancies. MAP2K1 L115P is a mutant of MAP2K1. MAP2K1 L115P Recombinant Human Active Protein Kinase is a recombinant MAP2K1 L115P protein that can be used to study MAP2K1 L115P-related functions.
    MAP2K1 L115P Recombinant Human Active Protein Kinase
  • HY-13078S
    Cobimetinib-13C6 racemate
    		Inhibitor
    Cobimetinib-13C6 (GDC-0973-13C6; XL518-13C6) racemate is the deuterium labeled Cobimetinib (racemate) (HY-13078). Cobimetinib racemate (GDC-0973 racemate; XL518 racemate) is the racemate of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
    Cobimetinib-<sup>13</sup>C<sub>6</sub> racemate
  • HY-172803
    Ferroptosis inducer-7
    		Activator
    Ferroptosis inducer-7 is an orally active and selective ferroptosis inducer via inositol 1,4,5-trisphosphate receptor (IP3R)/calcium release-activated calcium channel protein (ORAI). Ferroptosis inducer-7 exhibits a notable effect in alleviating anemia symptoms, suppressing bone marrow CTLs activation, and improving hematopoietic function in immune-mediated bone marrow failure. Ferroptosis inducer-7 can be studied in research for aplastic anemia.
    Ferroptosis inducer-7
  • HY-14584
    PQ-1
    		Modulator
    PQ-1 is a gap junction enhancer.
    PQ-1
  • HY-175235
    MEK4 IN-3
    		Inhibitor
    MEK4 IN-3 (Compound 39) is a selective MEK4 inhibitor with IC50s of 78   and 2920 nM for MEK4 and RSK4, respectively. MEK4 IN-3 reduces toxicity in cells. MEK4 IN-3 can be used for liver failure, particularly nonalcoholic fatty liver disease (NAFLD) research.
    MEK4 IN-3
  • HY-RS08037
    Map2k2 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Map2k2 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map2k2 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k2 Mouse Pre-designed siRNA Set A
  • HY-RS08036
    MAP2K2 Human Pre-designed siRNA Set A
    		Inhibitor

    MAP2K2 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MAP2K2 Human Pre-designed siRNA Set A
  • HY-N13009
    MO-2097
    		Inhibitor
    MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.
    MO-2097
  • HY-126180
    BAY-866
    		Inhibitor
    BAY-866, a sulfamide campound, is an allosteric MEK1 inhibitor with an IC50 of 14 nM. BAY-866 inhibits cell growth of A375 (BRAF) and HCT116 (K-Ras) with IC50s of 13 nM and 277 nM, respectively. BAY-866 inhibits tumor growth in K-Ras-mutated A549 xenograft model.
    BAY-866
  • HY-173153
    BRAFV600E/JNK-IN-1
    		Inhibitor
    BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities.
    BRAFV600E/JNK-IN-1
  • HY-120281
    ST-168
    		Inhibitor
    ST-168 is an orally active MEK/PI3K inhibitor with an IC50 of 182 nM against MEK1 and IC50 values ​​of 69.2, 41.7, 1482 and 2293 nM against PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ respectively. ST-168 completely inhibits the phosphorylation of ERK1/2 and AKT and induces cancer cell death in a 3D tumor sphere model. ST-168 demonstrates significant antitumor effects in the A375 melanoma mouse model. ST-168 improves the ocular toxicity profile of MEK inhibitors, showing lower caspase activation levels, indicating reduced apoptosis induction. ST-168 can be used in melanoma research.
    ST-168
  • HY-12447
    SMK-17
    		Inhibitor
    SMK-17 is a selective, non-ATP-competitive MEK1/MEK2 inhibitor with IC50s of 62 nM and 56 nM, respectively. SMK-17 binds to the allosteric pocket of MEK1/2. SMK-17 induces apoptosis in tumor cell lines harboring β-catenin mutations.
    SMK-17
  • HY-RS08038
    Map2k2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Map2k2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map2k2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k2 Rat Pre-designed siRNA Set A
  • HY-10508
    (R)-PD 0325901CL
    		Inhibitor
    (R)-PD 0325901CL is an isomer of PD 0325901CL. PD 0325901CL is a selective inhibitor of mitogen-activated protein kinase kinase (MEK) involved in cancer research. PD 0325901CL inhibits the growth of cancer cells in vitro and in vivo.
    (R)-PD 0325901CL
  • HY-12482
    X-370
    		Inhibitor
    X-370 is a PI3Kδ inhibitor (IC50 = 7 nM). X-370 inhibits the survival of leukemia cells, inducing G1 arrest and apoptosis. X-370 blocks PDK1 binding and phosphorylation of MEK1/2, eliminating Akt and Erk1/2 signaling. X-370 can be used in research on B-cell acute lymphoblastic leukemia (B-ALL).
    X-370
  • HY-RS08042
    Map2k5 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Map2k5 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Map2k5 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k5 Mouse Pre-designed siRNA Set A
  • 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-118626
    PD-254552
    		Inhibitor
    PD-254552 is a MEK inhibitor. PD-254552 exhibits hepatotoxicity and gastrointestinal toxicity in mice.
    PD-254552
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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