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-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-123586
    L-783277
    		Inhibitor
    L-783277 (Compound 4) is a MEK inhibitor (IC50 = 4 nM). L-783277 has potent inhibitory activity against a variety of kinases, including VEGFR2/3, FLT1/3/4, MEK1/2, KDR, and PDGFRα, but has low selectivity for the kinase community. L-783277 inhibits viability (IC50 = 22 mM) and cell proliferation (IC50 = 21 mM) of H295R cells. L-783277 could be used in research on cancers such as adrenocortical carcinoma.
    L-783277
  • 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-177081
    Envometinib
    		Inhibitor
    Envometinib (Compound B) is a dual-MEK inhibitor that works through Deep Cyclic Inhibition (DCI). Envometinib has antitumor activity in various in vivo models. Envometinib can be studied in RAS and RAF mutated cancer such as colorectal cancer and melanoma.
    Envometinib
  • HY-E70843
    MAP2K1 P124L Recombinant Human Active Protein Kinase
    MAP2K1 encodes mitogen-activated protein kinase 1 (MEK1), which is a key component in the RAS-mitogen-activated protein kinase kinase (RAS/MAPK) signal transduction pathway. MAP2K1 P124L mutation is a mild mutation. MAP2K1 P124L Recombinant Human Active Protein Kinase is a recombinant MAP2K1 P124L protein that can be used to study MAP2K1 P124L-related functions.
    MAP2K1 P124L Recombinant Human Active Protein Kinase
  • 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
  • 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-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
  • HY-111033
    RO5068760
    		Inhibitor
    RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research.
    RO5068760
  • HY-E70744
    MEK1 F53L 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 F53L is a mutant of MEK1. MEK1 F53L Recombinant Human Active Protein Kinase is a recombinant MEK1 F53L protein that can be used to study MEK1 F53L-related functions.
    MEK1 F53L Recombinant Human Active Protein Kinase
  • HY-RS08033
    MAP2K1 Human Pre-designed siRNA Set A
    		Inhibitor

    MAP2K1 Human Pre-designed siRNA Set A contains three designed siRNAs for MAP2K1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    MAP2K1 Human Pre-designed siRNA Set A
  • HY-153858
    PHI-501
    		Inhibitor
    PHI-501 is a dual inhibitor targeting RAF/DDR. PHI-501 exhibits significant anti-proliferative effects in melanoma cell lines and significantly inhibits the colony formation of drug-resistant cells. PHI-501 strongly inhibits ERK and AKT phosphorylation. PHI-501 downregulates the gene sets in drug-resistant cells of TNFA-NFKB, IL6-JAK-STAT3, and KRAS signaling pathways as well as the epithelial-mesenchymal transition (EMT) signaling pathways. PHI-501 demonstrates significant anti-tumor effects in the SK-MEL3DR xenograft model. PHI-501 can be used for research on the problem of drug resistance in melanoma.
    PHI-501
  • HY-P4133
    MEK1 Derived Peptide Inhibitor 1
    MEK1 Derived Peptide Inhibitor 1 is a peptide inhibitor. MEK1 Derived Peptide Inhibitor 1 can inhibit the in vitro activation of ERK2 by MEK1 with an IC50 value of 30 μM. MEK1 Derived Peptide Inhibitor 1 can be used for the research of cell-permeable.
    MEK1 Derived Peptide Inhibitor 1
  • HY-115674
    ML175
    		Activator
    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-162873
    MEK/RAF-IN-1
    		Inhibitor
    MEK/RAF-IN-1 (Compound 16b) is an inhibitor of both MEK and RAF. It shows potent inhibition with IC50 values of 28 nM for MEK1, and 3 nM each for BRAF and BRAFV600E. MEK/RAF-IN-1 demonstrates significant antitumor activity, effectively inhibiting cell proliferation in vitro against MIA PaCa-2 (G12C KRAS), HCT116 (G13D KRAS), and C26 (G12D KRAS) cells. Additionally, it inhibits tumor growth in xenograft mouse models of colorectal cancer.
    MEK/RAF-IN-1
  • HY-170982
    MS910
    		Inhibitor
    MS910 is an efficient and selective MEK1/2 PROTAC degrader. MS910 exhibits effective MEK1/2 degradation ability and anti proliferative activity in various cancer cells, such as HT-29 (MEK1 DC50 = 118 nM, MEK2 DC50 = 55 nM) and SK-MEL-28 (MEK1 DC50 = 94 nM, MEK2 DC50 = 38 nM) cells. MS910 is commonly used in cancer research. (Pink: MEK1/2 Ligand (HY-10254); Blue: CRBN Ligand (HY-W087383); Black: Linker (HY-W022240))
    MS910
  • HY-139639
    MEK4 inhibitor-2
    		Inhibitor
    MEK4 inhibitor-2 is a novel MEK4 inhibitor against pancreatic adenocarcinoma with an IC50 value of 83 nM.
    MEK4 inhibitor-2
Cat. No. Product Name / Synonyms Application Reactivity
MEK Isoform Comparison

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