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-107621
    U0124
    		98.0%
    U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM.
    U0124
  • HY-10174
    PD184161
    		Inhibitor 98.08%
    PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior.
    PD184161
  • HY-N1988
    Cucurbitacin IIa
    		Inhibitor 99.90%
    Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC50 of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.
    Cucurbitacin IIa
  • HY-B1853
    Simetryn
    		Activator 99.75%
    Simetryn is a triazine herbicide that exerts teratogenicity. Simetryn inhibits photosynthesis by blocking electron transfer in the chloroplast photosystem II and activates the MEK/Erk signaling pathway. Simetryn triggers vascular and developmental abnormalities in zebrafish and tadpoles, suppresses proliferation, enhances apoptosis, and induces malformations. Simetryn serves as a tool to establish a zebrafish model for studying arteriovenous malformations and related pathogenesis. Simetryn controls paddy weeds and can be used for research on developmental and vascular disorders.
    Simetryn
  • HY-156625
    Nedometinib
    		Inhibitor 98.09%
    Nedometinib (NFX-179) is a specific MEK1 inhibitor with an IC50 of 135 nM. Nedometinib inhibits p-ERK, MAPK. Nedometinib exerts anticancer activity against squamous cell carcinoma. Nedometinib can be used for research in dermatosis, neurofibromatosis.
    Nedometinib
  • HY-160142
    UBX-382
    		Inhibitor
    UBX-382 is an orally active BTK PROTAC degrader with a DC50 of 4.56 nM. UBX-382 inhibits B-cell receptor signaling by targeting BTK. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins. UBX-382 inhibits tumor growth in murine xenograft models harboring wild-type or C481S mutant BTK-expressing TMD-8 cells. UBX-382 can be used for the study of B-cell-related blood cancers.
    UBX-382
  • HY-12202
    MEK inhibitor
    		Inhibitor 98.35%
    MEK inhibitor is a potent MEK inhibitor with antitumor potency.
    MEK inhibitor
  • HY-107417
    Hypothemycin
    		Inhibitor 98.0%
    Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively.
    Hypothemycin
  • HY-148507
    GSK1790627
    		Inhibitor 99.08%
    GSK1790627 is the N-deacetylated metabolite of Trametinib (HY-10999). Trametinib is an orally active MEK inhibitor, and activates autophagy and induces apoptosis.
    GSK1790627
  • HY-13079
    Cobimetinib (R-enantiomer)
    		Inhibitor 99.78%
    Cobimetinib R-enantiomer is the less active R-enantiomer of Cobimetinib. Cobimetinib is a potent and selective MEK inhibitor.
    Cobimetinib (R-enantiomer)
  • HY-10999S
    Trametinib-d4
    		Inhibitor 99.87%
    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-177511
    KRAS G12D-IN-30
    		Inhibitor 99.38%
    KRAS G12D-IN-30 (Compound 4) is a KRAS inhibitor. KRAS G12D-IN-30 inhibits the activation of the downstream MAPK signaling cascade (Raf1-MEK-ERK) by blocking the activity of the KRAS G12 mutant. KRAS G12D-IN-30 can be used for the research of cancer.
    KRAS G12D-IN-30
  • HY-13064S1
    Cobimetinib-d4 hydrochloride
    		Inhibitor 99.26%
    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-14947
    Balamapimod
    		Inhibitor 99.47%
    Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
    Balamapimod
  • HY-115674
    ML175
    		Activator 99.37%
    ML175 is a specific glutathione transferase Omega 1-1 (GSTO1-1) inhibitor. ML175 can significantly activate Akt and MEK1/2 kinases. ML175 can be used in the research of diseases such as Parkinson's disease.
    ML175
  • HY-W357818
    Glycinexylidide
    		Inhibitor
    Glycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local agent that can suppress or relieve pain, that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
    Glycinexylidide
  • HY-101481
    Flurbiprofen axetil
    		Inhibitor 99.34%
    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
  • HY-153864
    PROTAC MEK1 Degrader-1
    		Inhibitor 98.28%
    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-107619
    PD-334581
    		Inhibitor 99.72%
    PD-334581 is a MEK1 inhibitor.
    PD-334581
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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