1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. MEK

MEK

MEK (Mitogen-activated protein kinase kinase, MAPKK) is a kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). The activators of p38 (MKK3 and MKK6), JNK (MKK4 and MKK7), and ERK (MEK1 and MEK2) define independent MAP kinase signal transduction pathways. The acronym MEK derives from Mitogen/Extracellular signal-regulated Kinase. MEK is a member of the MAPK signaling cascade that is activated in melanoma. When MEK is inhibited, cell proliferation is blocked and apoptosis (controlled cell death) is induced.

MEK Isoform Specific Products:

  • MEK1

  • MEK2

  • MEK5

  • MEK

MEK Related Products (41):

Cat. No. Product Name Effect Purity
  • HY-12031
    U0126 98.06%
    U0126 is a potent and non-ATP competitive MEK1 and MEK2 inhibitor, with IC50s of 70 nM and 60 nM, respectively.
  • HY-12028
    PD98059 Inhibitor 99.33%
    PD98059 is a potent, selective and cell-permeable MEK1 and MEK2 inhibitor with IC50s of 4 μM and 50 μM respectively.
  • HY-10999
    Trametinib Inhibitor 99.44%
    Trametinib is a potent MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Due to the poor solubility of Trametinib, Trametinib DMSO solvate (Cat. No.: HY-10999A) is recommeded.
  • HY-10254
    PD0325901 Inhibitor 99.95%
    PD0325901 is a selective and cell permeable MEK inhibitor with an IC50 of 0.33 nM.
  • HY-50706
    Selumetinib Inhibitor 99.87%
    Selumetinib is a highly potent MEK inhibitor, with an IC50 of 14 nM against MEK1.
  • HY-114189
    GW284543 Inhibitor 99.86%
    GW284543 (UNC10225170) is a selective MEK5 inhibitor. GW284543 (UNC10225170) reduces pERK5, and decreases endogenous MYC protein.
  • HY-101522
    CHMFL-EGFR-202 Inhibitor
    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.
  • HY-111368
    EBI-1051 Inhibitor
    EBI-1051 is a highly potent and orally efficacious MEK inhibitor with an IC50 of 3.9 nM.
  • HY-10999A
    Trametinib DMSO solvate Inhibitor 99.77%
    Trametinib DMSO solvate is a potent MEK inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.
  • HY-13064
    Cobimetinib Inhibitor 99.38%
    Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1.
  • HY-15202
    Binimetinib Inhibitor 98.61%
    Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
  • HY-50295
    CI-1040 Inhibitor 98.54%
    CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-18652
    Ro 5126766 Inhibitor
    Ro 5126766 is a first-in-class dual MEK/RAF inhibitor that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF (IC50: 8.2, 56, 160 nM, and 190 nM, respectively).
  • HY-B0185
    Lidocaine Inhibitor 99.52%
    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 a commonly used local anesthetics of amide derivative, a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-12042
    Pimasertib Inhibitor 99.95%
    Pimasertib (AS703026) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2, used for cancer treatment.
  • HY-15504A
    RGB-286638 free base Inhibitor 98.07%
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
  • HY-N0776
    Isorhamnetin Inhibitor 99.95%
    Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and PI3K.
  • HY-B0185A
    Lidocaine hydrochloride Inhibitor 99.95%
    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 a commonly used local anesthetics of amide derivative, a drug to treat ventricular arrhythmia and an effective tumor-inhibitor.
  • HY-15437
    SL327 Inhibitor >98.0%
    SL327 inhibits MEK1 and MEK2, with IC50 values of 180 nM and 220 nM, respectively.
  • HY-12056
    BIX02189 Inhibitor 99.99%
    BIX02189 is a potent and selective MEK5 inhibitor with an IC50 of 1.5 nM. BIX02189 also inhibits ERK5 catalytic activity with an IC50 of 59 nM.
Isoform Specific Products

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