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


MAPK Kinase Kinase Kinase

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.

Cat. No. Product Name Effect Purity
  • HY-100830
    Inhibitor 99.61%
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
  • HY-100343
    Inhibitor 99.40%
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
  • HY-111754
    Inhibitor 99.63%
    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-138568
    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-135892
    Inhibitor 99.42%
    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-146231A
    SS47 TFA
    Inhibitor 99.88%
    SS47 TFA, a PROTAC-based HPK1 degrader, exerts proteasome-mediated HPK1 degradation. The degradation of HPK1 via SS47 also significantly enhances the in vivo antitumor efficacy of BCMA CAR-T cell research. HPK1, an immunosuppressive regulatory kinase, is a promising target for cancer immunotherapies. SS47 (TFA) is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • HY-15434A
    NG25 trihydrochloride
    NG25 trihydrochloride is a dual TAK1 and MAP4K2 inhibitor (IC50: 149 nM and 21.7 nM respectively). NG25 sensitizes the breast cancer cells to Doxorubicin (HY-15142A), and enhances apoptosis. NG25 trihydrochloride can be used for research of various cancers.
  • HY-153553
    HPK1 antagonist-1
    HPK1 antagonist-1 (I-792) is an Hpk1 antagonist that can be used in the study of cancer and immune disease.
  • HY-138742
    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-15434
    Inhibitor 99.35%
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
  • HY-19562
    Inhibitor 99.67%
    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-124745
    Inhibitor 99.24%
    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-125012
    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-148847
    Inhibitor 98.12%
    HPK1-IN-32 is a potent and selective HPK1 inhibitor with an IC50 of 65 nM. HPK1-IN-32 can be used for the research of HPK1 related disorders or diseases.
  • HY-138569
    Inhibitor 99.09%
    HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunoresearch tool compound.
  • 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-132926
    Inhibitor 98.56%
    HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.
  • HY-77251
    TAK1/MAP4K2 inhibitor 1
    Inhibitor 98.07%
    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-144088
    Inhibitor ≥98.0%
    ZYF0033 (HPK1-IN-22, compound ZYF0033) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 decreases the phosphorylation of SLP76 (serine 376). ZYF0033 promotes anticancer immune responses. ZYF0033 inhibits tumor growth and caused increases intratumoral infiltration of DCs, NK cells, and CD107a+CD8+ T cells but decreased infiltration of regulatory T cells, PD-1+CD8+ T cells, TIM-3+CD8+ T cells, and LAG3+CD8+ T cells in the 4T-1 syngeneic mouse model.
  • HY-144093
    Inhibitor ≥98.0%
    HPK1-IN-26 is a HPK1 and GLK inhibitor extracted from patent WO2021254118A1 compound 1. HPK1-IN-26 can be used for the research of animal pathogen infection.

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