1. MAPK/ERK Pathway
  2. 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 Related Products (28):

Cat. No. Product Name Effect Purity
  • HY-12031
    U0126 Inhibitor
    U0126 is a non-ATP competitive MEK inhibitor, with IC50 of 70 nM and 60 nM for MEK1 and MEK2, respectively.
  • HY-10999
    Trametinib Inhibitor
    Trametinib is a potent MEK1/2 inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.
  • HY-12028
    PD98059 Inhibitor
    PD98059 is an MEK inhibitor with IC50 of 5 μM, also suppresses TCDD binding to the aryl hydrocarbon receptor (AHR) with IC50 of 4 μM.
  • HY-50706
    Selumetinib Inhibitor
    Selumetinib is a highly potent MEK inhibitor, with an IC50 value of 14 nM against MEK1.
  • HY-10254
    PD0325901 Inhibitor
    PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2.
  • HY-13064
    Cobimetinib Inhibitor
    Cobimetinib is a novel selective MEK inhibitor, and the IC50 value against MEK1 is 4.2 nM.
  • HY-10999A
    Trametinib DMSO solvate Inhibitor
    Trametinib DMSO solvate is a potent MEK1/2 inhibitor that specifically inhibits MEK1/2, with an IC50 value of about 2 nM.
  • HY-15202
    MEK162 Inhibitor
    MEK162 is a potent and selective mitogen-activated protein kinase (MEK) inhibitor wirh IC50 of 12 nM.
  • HY-N0003
    Honokiol Activator
    Honokiol is a hydroxylated biphenyl compound, which inhibits the activation of Akt and enhances the phosphorylation of ERK1/2.
  • HY-50295
    CI-1040 Inhibitor
    CI-1040 (PD184352) is an orally active, highly specific, small-molecule inhibitor of MEK with an IC50 of 17 nM for MEK1.
  • HY-14691
    Refametinib Inhibitor
    Refametinib (RDEA119, BAY 86-9766), is an orally bioavailable selective MEK inhibitor with potential antineoplastic activity (IC50=19 nM MEK1; IC50=47 nM MEK2).
  • HY-15610
    GDC-0623 Inhibitor
    GDC-0623 is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAFV600E, EC50=7 nM).
  • HY-12467
    OTS-964 Inhibitor
    OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM.
  • HY-12042
    AS703026 Inhibitor
    AS703026(Pimasertib) is a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2 with IC50 of 5 nM-2 μM in MM cell lines.
  • HY-12056
    BIX02189 Inhibitor
    BIX02189 is a selective MEK5/ERK5 inhibitor with an IC50 of 59 nM.
  • HY-18652
    Ro 5126766 Inhibitor
    Ro 5126766 (CH5126766) is a potent and selective dual RAF/MEK inhibitor. For SK-MEL-28, SK-MEL-2, MIAPaCa-2, and SW480 cell lines, the IC50 is determined by WST-8 assay is 65, 28, 40, and 46 nM, respectively.
  • HY-13449
    TAK-733 Inhibitor
    TAK-733 is a potent and selective MEK allosteric site inhibitor for MEK1 with IC50 of 3.2 nM, inactive to Abl1, AKT3, c-RAF, CamK1, CDK2, c-Met, etc.
  • HY-12058
    AZD8330 Inhibitor
    AZD8330(ARRY-424704; ARRY-704) is a novel, selective, non-ATP competitive MEK 1/2 inhibitor with IC50 of 7 nM.
  • HY-14719
    RO4987655 Inhibitor
    RO4987655(CH-4987655) is an orally active small molecule, targeting mitogen-activated protein kinase kinase 1 (MAP2K1/MEK1 IC50=5.2 nM), with potential antineoplastic activity.
  • HY-12055
    BIX02188 Inhibitor
    BIX02188 is a selective inhibitor of MEK5 with IC50 of 4.3 nM, also inhibits ERK5 catalytic activity with IC50 of 810 nM, and does not inhibit closely related kinases MEK1, MEK2, ERK2, and JNK2.