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

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 Chemical Structure
  • HY-170443
    PF-07265028
    Inhibitor
    PF-07265028 is a selective hematopoietic progenitor kinase 1 (HPK1/MAP4K1). PF-07265028 can be used in the research of cancer. PF-07265028 shows very potent cellular activity as measured by pSLP76 IC50 (17 nM).
    PF-07265028
  • HY-156508
    HPK1-IN-37
    Inhibitor
    HPK1-IN-37 (compound A85) is an inhibitor of HPK1 (IC50=3.7 nM). HPK1-IN-37 can be used for research in HPK1 related disorders or diseases including cancers.
    HPK1-IN-37
  • HY-169199
    BAY-405
    Inhibitor
    BAY-405 (compund 38) is a MAP4K1 inhibitor that exhibits nanomolar potency in biochemical and cellular assays and achieves in vivo exposure after oral administration.
    BAY-405
  • HY-143871
    HPK1-IN-30
    Inhibitor
    HPK1-IN-30 is a potent inhibitor of HPK1. MAP4K1 is also known as hematopoietic progenitor kinase 1 (HPK1). MAP4K1 is a serine/threonine kinase and member of the germinal center kinase family. HPK1-IN-30 has the potential for the research of cancer diseases (extracted from patent WO2021175271A1, compound 3).
    HPK1-IN-30
  • HY-168282
    DD205-291
    Degrader
    DD205-291 is an orally active PROTAC HPK1 degrader, with a DC50 value of 5.3 nM. DD205-291 inhibits SLP-76 phosphorylation and induces IL-2 and IFN-γ expression (Pink: HPK1 protein ligand HY-168283; E3+linker: HY-168284; Blue: E3: HY-W115490; Black: linker: HY-W210252).
    DD205-291
  • HY-149206
    HPK1-IN-33
    Inhibitor
    HPK1-IN-33 (compound 21) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a Ki value of 1.7 nM. HPK1-IN-33 inhibits the produce of IL-2 with EC50s of 286, >10000 nM in Jurkat WT and Jurkat HPK1 KO cells, respectively.
    HPK1-IN-33
  • HY-170365
    HPK1-IN-55
    Inhibitor
    HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <0.51 nM. HPK1-IN-55 shows excellent kinase selectivity (>637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects.
    HPK1-IN-55
  • HY-160218
    HPK1-IN-42
    Inhibitor
    HPK1-IN-42 (compound 185) ia a HPK1 inhibitor with the IC50 50 of 0.24 nM.
    HPK1-IN-42
  • HY-15434R
    NG25 (Standard)
    Inhibitor
    NG25 (Standard) is the analytical standard of NG25. This product is intended for research and analytical applications. NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
    NG25 (Standard)
  • HY-159905
    HPK1-IN-54
    Inhibitor
    HPK1-IN-54 is a potent HPK1 (Hematopoietic Progenitor Kinase 1) inhibitor that enhances T cell activation and proliferation by inhibiting HPK1 activity, thereby exhibiting antitumor effects. Its IC50 value against HPK1 is 2.67 nM, with excellent selectivity over the MAP4K family (>100-fold) and other selected kinases (>300-fold). HPK1-IN-54 displayed moderate in vivo clearance and reasonable oral exposure in mice and rats. Additionally, HPK1-IN-54 demonstrated strong antitumor efficacy in a CT26 murine colon cancer model and synergistic effects when combined with anti-PD-1 (HY-P9902A). HPK1-IN-54 shows promise for research in the field of immunotherapy.
    HPK1-IN-54
  • HY-163717
    HPK1-IN-48
    Inhibitor
    HPK1-IN-48 (compound 14g) is a potent Hematopoietic Progenitor Kinase 1 (HPK1) inhibitor with a IC50 of 0.15 nM. HPK1-IN-48 significantly suppresses the phosphorylation of SLP76 with a IC50 of 27.92 nM.
    HPK1-IN-48
  • HY-161335
    HPK1-IN-43
    Inhibitor
    HPK1-IN-43 (compound 9f) is a HPK1 kinase inhibitor with the IC50 value of 0.32 nM. HPK1-IN-43 inhibits the phosphorylation of the downstream protein SLP-76 and enhances the secretion of interleukin-2 (IL-2) and interferon-γ (IFN-γ). HPK1-IN-43 can be used in cancer research.
    HPK1-IN-43
  • HY-144091
    HPK1-IN-24
    Inhibitor
    HPK1-IN-24 (example 51) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a Ki of 100 nM. HPK1-IN-24 has the potential for cancer research.
    HPK1-IN-24
  • HY-19562A
    PF-06260933 hydrochloride
    Inhibitor
    PF-06260933 hydrochloride is the hydrochloride form of PF-06260933 (HY-19562). PF-06260933 hydrochloride 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 hydrochloride
  • HY-168119
    HPK1-IN-53
    Inhibitor
    HPK1-IN-53 (compund 3a) is the potent HPK1 inhibitor (IC50=48 nM).
    HPK1-IN-53
  • HY-144092
    HPK1-IN-25
    Inhibitor
    HPK1-IN-25 (example 94) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with a enzymatic activity IC50 of 129 nM. HPK1-IN-25 has the potential for cancer research.
    HPK1-IN-25

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