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

MAP4K

MAPK Kinase Kinase Kinase

MAP4K

Related Products

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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:

MAP4K Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100830
    NCB-0846
    		Inhibitor 99.61%
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
    NCB-0846
  • HY-100343
    GNE-495
    		Inhibitor 99.40%
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
    GNE-495
  • HY-111754
    DMX-5804
    		Inhibitor 99.83%
    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.
    DMX-5804
  • 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.
    NG25
  • HY-19562
    PF-06260933
    		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.
    PF-06260933
  • HY-159643
    NDI-101150
    		Inhibitor
    NDI-101150 is an orally active, potent and selective hematopoietic progenitor cell kinase 1 (HPK1) inhibitor. NDI-101150 enhances T cell activation and inhibits tumor growth.
    NDI-101150
  • HY-162816
    PROTAC HPK1 Degrader-3
    PROTAC PD-L1 degrader-2 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC PD-L1 degrader-2 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC PD-L1 degrader-2 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC PD-L1 degrader-2 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841)[1].
    PROTAC HPK1 Degrader-3
  • HY-162544
    PROTAC HPK1 Degrader-2
    		Degrader
    PROTAC HPK1 Degrader-2 (compound 3) is a PROTAC degrader of HPK1, with the DC50 of 23 nM in human PBMC. PROTAC HPK1 Degrader-2 plays an important role in cancer research.
    PROTAC HPK1 Degrader-2
  • HY-138568
    HPK1-IN-3
    		Inhibitor 99.32%
    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).
    HPK1-IN-3
  • HY-124745
    KY-05009
    		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.
    KY-05009
  • HY-138742
    HPK1-IN-7
    		Inhibitor 99.33%
    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.
    HPK1-IN-7
  • HY-135892
    GNE-1858
    		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.
    GNE-1858
  • HY-157149
    DS21150768
    		Inhibitor 99.26%
    DS21150768 is a potent, orally active HPK1 inhibitor. DS21150768 shows potent activity to enhance T-cell function. DS21150768 has anticancer effects.
    DS21150768
  • HY-148847
    HPK1-IN-32
    		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.
    HPK1-IN-32
  • HY-144088
    ZYF0033
    		Inhibitor 98.86%
    ZYF0033 is effective in inhibiting hematopoietic progenitor cells HPK1, basically inhibiting MBP protein oxidation IC50 10 nM . ZYF0033 promotes anti-cancer immune response, lowers SLP76 (acid 376) oxidation. ZYF0033 Suppression 4T-1 Small mouse model with the same underlying cause, medium bulge growth length expansion DC, NK 细细和 CD107a+ CD8+ T Cells, PD-1+CD8+ T Cells, TIM-3+CD8+ T Cells LAG3< sup>+CD8+ T Cellular immersion decreases.
    ZYF0033
  • HY-125012
    MAP4K4-IN-3
    		Inhibitor 99.15%
    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.
    MAP4K4-IN-3
  • HY-U00428A
    GNE 220 hydrochloride
    		Inhibitor 98.22%
    GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.
    GNE 220 hydrochloride
  • HY-160623
    INS018 055
    		Inhibitor 99.38%
    INS018 055 (compound 112) is a TNIK and MAP4K4 inhibitor with IC50 values of 12-120, 12-120 nM, respectively.
    INS018 055
  • 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, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    SS47 TFA
  • HY-123714
    TL4-12
    		Inhibitor 99.82%
    TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC50=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).
    TL4-12
MAP4K Isoform Comparison

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