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-160623
    Rentosertib
    		Inhibitor 99.96%
    Rentosertib (INS018 055) (compound 112) is the orally active TNIK and MAP4K4 inhibitor with IC50 values of 12-120, 12-120 nM, respectively.
    Rentosertib
  • HY-100343
    GNE-495
    		Inhibitor 99.49%
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
    GNE-495
  • HY-100830
    NCB-0846
    		Inhibitor 99.61%
    NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation.
    NCB-0846
  • HY-19562
    PF-06260933
    		Inhibitor 99.39%
    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-15434
    NG25
    		Inhibitor 98.68%
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
    NG25
  • HY-181924
    HPK1-IN-68
    		Inhibitor
    HPK1-IN-68 (Compound 39) is a HPK1 inhibitor with an IC50 of 2.8 nM. HPK1-IN-68 blocks HPK1 signaling, inhibits HPK1-mediated phosphorylation of SLP76, and promotes the production of the IL-2 cytokine. HPK1-IN-68 antagonizes the immunosuppressive effect mediated by PGE2. HPK1-IN-68 enhances the infiltration of CD3+/CD8+ T cells into tumor tissues. HPK1-IN-68 exerts T cell-dependent antitumor efficacy in a mouse colon cancer model. HPK1-IN-68 exhibits significant synergistic antitumor effects when used in combination with anti-PD-1. HPK1-IN-68 is applicable to research related to colon cancer.
    HPK1-IN-68
  • HY-181932
    HDM2004
    		Inhibitor
    HDM2004 is a selective, orally active, blood-brain barrier-penetrant HPK1 inhibitor with an IC50 of 1.89 nM. HDM2004 exhibits anticancer activity against colon cancer. HDM2004 shows synergistic activity when combined with anti-PD-L1 in syngeneic mouse models. HDM2004 can be used for the research of colon cancer.
    HDM2004
  • HY-182811
    AT-051/43421517
    AT-051/43421517 is a cytoprotective agent and apoptosis inhibitor that binds to human phosphoglycerate kinase 1 (hPgk1). AT-051/43421517 protects cells from rotenone-induced cell death without inducing cell proliferation. AT-051/43421517 can be used for the research of parkinson’s disease.
    AT-051/43421517
  • 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-124745
    KY-05009
    		Inhibitor 99.88%
    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-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-125012
    MAP4K4-IN-3
    		Inhibitor 99.77%
    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-138568
    HPK1-IN-3
    		Inhibitor 98.61%
    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-W058423
    6-Bromo-3-fluoropyridine-2-carbaldehyde
    		99.92%
    6-Bromo-3-fluoropyridine-2-carbaldehyde (synthetic intermediate of Compound I-90) is a synthetic intermediate. 6-Bromo-3-fluoropyridine-2-carbaldehyde can be used in the synthesis of HPK1 inhibitors. 6-Bromo-3-fluoropyridine-2-carbaldehyde is applicable to research on immune diseases and hematological diseases.
    6-Bromo-3-fluoropyridine-2-carbaldehyde
  • HY-168972
    Famlasertib
    		Inhibitor 99.94%
    Famlasertib is a potent, brain-penetrant MAP4K inhibitor with IC50s value of 0.3 nM, 23.7 nM, and 44.7 nM for HGK (MAP4K4), MLK3, and MLK1, respectively. Famlasertib shows motor neuron protection and anti-inflammatory properties. Famlasertib can be used for the study of amyotrophic lateral sclerosis (ALS).
    Famlasertib
  • HY-144088
    ZYF0033
    		Inhibitor 98.82%
    ZYF0033 is an orally active inhibitor of the hematopoietic progenitor cell kinase HPK1 with an IC50 of less than 10 nM based on the phosphorylation inhibition of MBP protein. ZYF0033 promotes anti-cancer immune responses and reduces phosphorylation of SLP76 (serine 376). ZYF0033 inhibits tumor growth in the 4T-1 syngeneic mouse model and leads to increased intratumoral infiltration of DCs, NK cells, and CD107a+CD8+ T cells, but not T cells, PD-1+CD8+ T cells, TIM-3+CD8+ Infiltration of T cells and LAG3+CD8+ T cells was reduced.
    ZYF0033
  • HY-N0894
    Octahydrocurcumin
    		Inhibitor 99.25%
    Octahydrocurcumin (Hexahydrobisdemethoxycurcumin) is an orally active anticancer and anti-inflammatory agent, and is the final hydrogenated metabolite of Curcumin (HY-N0005) in vivo. Octahydrocurcumin exerts its anti-tumor and anti-inflammatory effects by inducing the mitochondrial apoptosis pathway and inhibiting the TAK1-NF-κB-COX-2 pathway, respectively.
    Octahydrocurcumin
  • HY-148065
    FMF-06-098-1
    		Inhibitor 98.77%
    FMF-06-098-1 is a multi-target kinase PROTAC degrader. FMF-06-098-1 can be used to target degradation kinases which degrades AAK1, AΒL2, AURKA, AURKB, BUBIB, CDC7, CDK1, CDK12, CDK13, CDK2, CDK4, CDk6, CDK7, CDK9, CHEK1, CSNKID, EPHA1, PER, FGFR1, GAK, IRAK4, ITK, LIMK2, MAP4K2, MAP4K3, MAPK6, MAPK7, MARK4, MELK, PKN3, PLK4, PRKAA1, PTK2, PTK6, RPS6KA4, S1K2, STK35, TNK2, UHMK1, ULK1, and WEE1.
    FMF-06-098-1
  • HY-148847
    HPK1-IN-32
    		Inhibitor 98.72%
    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-77251
    TAK1/MAP4K2 inhibitor 1
    		Inhibitor 99.91%
    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.
    TAK1/MAP4K2 inhibitor 1
MAP4K Isoform Comparison

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