1. Signaling Pathways
  2. MAPK/ERK Pathway
  3. MAP4K

MAP4K

MAP kinase kinase kinase kinases (MAP4Ks) belong to the mammalian Ste20-like family of serine/threonine kinases. MAP4Ks including MAP4K1/HPK1, MAP4K2/GCK, MAP4K3/GLK, MAP4K4/HGK, MAP4K5/KHS, and MAP4K6/MINK have been reported to induce JNK activation through activating the MAP3K-MAP2K cascade. MAP4Ks play important roles in the regulation of cell apoptosis, cell survival, cell autophagy, and cell migration. Several studies reported that MAP4Ks are involved in the regulation of immune-cell responses through JNK-independent pathways.

MAP4K1/HPK1 and MAP4K4/HGK play negative roles in T-cell activation and inflammatory responses. In contrast, MAP4K3/GLK plays a positive role in T-cell activation and autoimmune responses. Moreover, MAP4K1 downregulation and MAP4K3 overexpression in T cells are involved in human autoimmune diseases such as psoriatic arthritis, rheumatoid arthritis (RA), adult-onset Still’s disease, and SLE.

MAP4K Isoform Specific Products:

  • MAP4K2/GCK

  • MAP4K3/GLK

  • MAP4K4/HGK

  • MAP4K5/KHS1

  • MAP4K6/MINK1

  • MAP4K7/TNIK

  • MAP4K1/HPK1

MAP4K Related Products (14):

Cat. No. Product Name Effect Purity
  • HY-135892
    GNE-1858
    Inhibitor 99.0%
    GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
  • HY-100830
    NCB-0846
    Inhibitor 99.36%
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
  • HY-111754
    DMX-5804
    Inhibitor 99.90%
    DMX-5804 is a potent, orally active and selective MAP4K4 inhibitor, with an IC50 of 3 nM, a pIC50 of 8.55 for human MAP4K4, less potent on MINK1/MAP4K6 (pIC50, 8.18), and TNIK/MAP4K7 (pIC50, 7.96). DMX-5804 enhances cardiomyocyte survival, and reduces ischemia-reperfusion injury in mice.
  • HY-100343
    GNE-495
    Inhibitor 99.68%
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
  • HY-19562
    PF-06260933
    Inhibitor 98.41%
    PF-06260933 is an orally active and highly selective inhibitor of MAP4K4 with IC50s of 3.7 and 160 nM for kinase and cell, respectively.
  • HY-138568
    HPK1-IN-3
    Inhibitor 98.53%
    HPK1-IN-3 is a potent and selective ATP-competitive hematopoietic progenitor kinase 1 (HPK1; MAP4K1) inhibitor with an IC50 of 0.25 nM. HPK1-IN-3 has IL-2 cellular potency with an EC50 of 108 nM in human peripheral blood mononuclear cells (PBMCs).
  • HY-138742
    HPK1-IN-7
    Inhibitor 99.61%
    HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1.
  • HY-138569
    HPK1-IN-4
    Inhibitor
    HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunotherapy tool compound.
  • 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-124745
    KY-05009
    Inhibitor 99.80%
    KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a Ki of 100 nM. KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.
  • HY-U00428A
    GNE 220 hydrochloride
    Inhibitor 98.33%
    GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
  • 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-125012
    MAP4K4-IN-3
    Inhibitor 99.13%
    MAP4K4-IN-3 (Compound 17) is a potent and selective MAP4K4 inhibitor with an IC50 of 14.9 nM in kinase assay, an IC50 of 470 nM in cell assay. Antidiabetic agent.
  • HY-U00428
    GNE 220
    Inhibitor
    GNE-220 is a potent and selective inhibitor of MAP4K4 with an IC50 of 7 nM.
Isoform Specific Products

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