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-122404
    Xantocillin
    		Inhibitor
    Xantocillin (Xanthocillin X) is a marine agent extracted from Penicillium commune, induces autophagy through inhibition of the MEK/ERK pathway.
    Xantocillin
  • HY-160414
    TRX-COBI
    		Inhibitor
    TRX-COBI ((R,R)-TRX-COBI; Trx-cobimetinib) is a MEK inhibitor targeting TRX fragments based on Fe2+. TRX-COBI has antitumor activity.
    TRX-COBI
  • HY-139638
    MEK4 inhibitor-1
    		Inhibitor 98.89%
    MEK4 inhibitor-1 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 61 nM.
    MEK4 inhibitor-1
  • HY-101522
    CHMFL-EGFR-202
    		Inhibitor 99.75%
    CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines.
    CHMFL-EGFR-202
  • HY-B0185G
    Lidocaine (GMP)
    		Inhibitor
    Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine 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.
    Lidocaine (GMP)
  • HY-N12740
    Napyradiomycin B4
    		Inhibitor
    Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis.
    Napyradiomycin B4
  • HY-100627A
    APS-2-79 hydrochloride
    		Antagonist
    APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATPbiotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling.
    APS-2-79 hydrochloride
  • HY-10999S
    Trametinib-d4
    		Inhibitor
    Trametinib-d4 is the 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-d<sub>4</sub>
  • HY-111368
    EBI-1051
    		Inhibitor
    EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
    EBI-1051
  • HY-12031B
    (2Z,3Z)-U0126
    (2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
    (2Z,3Z)-U0126
  • HY-N10092
    Saucerneol
    		Inhibitor
    Saucerneol is a lignans that can be isolated from Saururus chinensis. Saucerneol inhibits LPS-induced or Con A-induced lymphocytes proliferation. Saucerneol inhibits mixed lymphocyte response. Saucerneol also inhibits mitogens-induced cytokines secretion.
    Saucerneol
  • HY-RS08035
    Map2k1 Rat Pre-designed siRNA Set A
    		Inhibitor

    Map2k1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map2k1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k1 Rat Pre-designed siRNA Set A
    Map2k1 Rat Pre-designed siRNA Set A
  • HY-143468
    MEK-IN-5
    		Inhibitor
    MEK-IN-5 is a potent MEK inhibitor and NO donor. MEK-IN-5 significantly reduces the levels of pMEK and pERK in a dose-dependent and time-dependent manner. MEK-IN-5 induces apoptosis in MDA-MB-231 cells.
    MEK-IN-5
  • HY-18652A
    Avutometinib potassium
    		Inhibitor
    Avutometinib (CH5126766) (potassium) is a RAF/MEK clamp that potently inhibits RAF/MEK kinase activity and induces dominant negative RAF-MEK complexes preventing phosphorylation of MEK by ARAF, BRAF and CRAF. Avutometinib (potassium) shows anti-proliferative potency across tumor cell lines carrying KRAS mutations including PDAC cell lines. Avutometinib (potassium) induces tumor inhibition and increases survival in a KRAS/p53 pancreatic cancer mouse model. Avutometinib (potassium) is promising for research of low-grade-serous-ovarian-carcinoma (LGSOC), ovarian cancer and pancreatic ductal adenocarcinoma (PDAC).
    Avutometinib potassium
  • HY-B0185AS1
    Lidocaine-d6 hydrochloride
    		Inhibitor
    Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). 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-d<sub>6</sub> hydrochloride
  • HY-RS08043
    Map2k5 Rat Pre-designed siRNA Set A
    		Inhibitor

    Map2k5 Rat Pre-designed siRNA Set A contains three designed siRNAs for Map2k5 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Map2k5 Rat Pre-designed siRNA Set A
    Map2k5 Rat Pre-designed siRNA Set A
  • HY-13064S1
    Cobimetinib-d4 hydrochloride
    		Inhibitor
    Cobimetinib-d4 hydrochloride is deuterated labeled Cobimetinib (HY-13064). Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
    Cobimetinib-d<sub>4</sub> hydrochloride
  • HY-107622
    (E/Z)-BIX02188
    		Inhibitor
    (E/Z)-BIX02188 is a MEK5/ERK5 pathway inhibitor. (E/Z)-BIX02188 inhibits the catalytic function of purified MEK5 enzyme.(E/Z)-BIX02188 can be used for the role of MEK5/ERK5 pathway in various biological systems .
    (E/Z)-BIX02188
  • HY-114189A
    GW284543 hydrochloride
    		Inhibitor
    GW284543 (UNC10225170) hydrochloride is a selective MEK5 inhibitor. GW284543 reduces pERK5, and decreases endogenous MYC protein.
    GW284543 hydrochloride
  • HY-113632
    Debromohymenialdisine
    Debromohymenialdisine (10Z-Debromohymenialdisine) is a pyrrole alkaloid. Debromohymenialdisine has moderate inhibitory activity with an IC50 value of 881 nM in the initial Raf/MEK-1/MAPK signaling cascade assay. Debromohymenialdisine can be used for the research of proliferation and differentiation.
    Debromohymenialdisine
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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