1. MAPK/ERK Pathway
  2. MAP3K


MAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, provide specificity for stimulus-dependent activation of MAP2K-MAPK pathways through unique protein-protein interactions and phosphorylation of signaling effectors. The MAP3Ks are highly divergent in gene numbers and structure, including TAK1, ASK1, A-Raf and C-Raf.

MAPK system is a three-step sequential phosphorylation cascade which is composed of MAPK, MAP2K, and MAP3K. ERK, p38 MAPK, and JNK, which are known to be activated by mechanical stimuli, belong to the MAPK family. MAP3Ks function as “platforms to integrate MAPK signaling, and activation of multiple MAP3Ks provides the spatiotemporal regulation of the MAPK pathways, which induces a wide range of physiological responses required for determining cell fate, such as cytokine production, survival, differentiation and apoptosis”.

MAP3K Related Products (25):

Cat. No. Product Name Effect Purity
  • HY-12947
    GNE-3511 Inhibitor 99.85%
    GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases[1].
  • HY-32018
    Cot inhibitor-2 Inhibitor 99.22%
    Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM[1].
  • HY-12686
    5Z-7-Oxozeaenol Inhibitor
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
  • HY-18938
    Selonsertib Inhibitor
    Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
  • HY-103490
    Takinib Inhibitor 99.31%
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM)[1][2][3].
  • HY-152247
    DDO3711 Inhibitor
    DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research[1].
  • HY-115743
    TAK1-IN-3 Inhibitor
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
  • HY-15434
    NG25 Inhibitor 99.35%
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
  • HY-114332
    GNE-8505 Inhibitor
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK)[1].
  • HY-112136
    TAO Kinase inhibitor 1 Inhibitor 99.29%
    TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death[1].
  • HY-131969
    ASK1-IN-2 Inhibitor 98.49%
    ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis[1].
  • HY-122232
    SW083688 Inhibitor
    SW083688 is a potent, highly selective TAOK2 (Thousand-And-One Kinase 2) inhibitor (IC50 values = 1.3 umol/L)[1].
  • HY-12358
    Tpl2 Kinase Inhibitor 1 Inhibitor
    Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers[1][2].
  • HY-77251
    TAK1/MAP4K2 inhibitor 1 Inhibitor 99.70%
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
  • HY-32015
    Cot inhibitor-1 Inhibitor 98.13%
    Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM[1].
  • HY-122642
    TAK1-IN-4 Inhibitor 99.47%
    TAK1-IN-4 (Compound 14) is a TAK1 inhibitor[1].
  • HY-124953
    7,3',4'-Trihydroxyisoflavone Inhibitor 99.98%
    7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities[1][2].
  • HY-114331
    DLK-IN-1 Inhibitor 99.41%
    DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
  • HY-103258
    TC ASK 10 Inhibitor
    TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM)[1].
  • HY-100844
    GS-444217 Inhibitor 99.67%
    GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM[1].