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-149773S
    HPK1-IN-40-d2
    Inhibitor
    HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity.
    HPK1-IN-40-d<sub>2</sub>
  • HY-163495
    HPK1-IN-44
    Inhibitor
    HPK1-IN-44 (Compound 1) is an inhibitor of HPK1 (IC50=0.1 nM (40 μM ATP)).
    HPK1-IN-44
  • HY-143869
    HPK1-IN-28
    Inhibitor
    HPK1-IN-28 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-28 enhances the body's anti-tumor immunity. HPK1-IN-28 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 1).
    HPK1-IN-28
  • HY-149232
    HPK1-IN-35
    Inhibitor
    HPK1-IN-35 is a potent and selective HPK1 inhibitor with an IC50 value of 3.5 nM. HPK1-IN-35 decreases the expression of p-SLP76 and promotes IL-2 secretion.
    HPK1-IN-35
  • HY-161917
    HPK1-IN-49
    Inhibitor
    HPK1-IN-49 (Compound I-4) is an inhibitor for hematopoietic progenitor kinase 1 (HPK1) with an IC50 >100 nM.
    HPK1-IN-49
  • HY-156523
    TNIK&MAP4K4-IN-1
    TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM,respectively,in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition.
    TNIK&MAP4K4-IN-1
  • HY-143870
    HPK1-IN-29
    Inhibitor
    HPK1-IN-29 is a potent inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPK1) is a negative regulator of the activation response of dendritic cells (DCs), T cells and B cells. HPK1-IN-29 enhances the body's anti-tumor immunity. HPK1-IN-29 has the potential for the research of immune-related diseases, especially tumor (extracted from patent WO2021175270A1, compound 38).
    HPK1-IN-29
  • HY-162545
    HPK1-IN-47
    Inhibitor
    HPK1-IN-47 is a HPK1 ligand. HPK1-IN-47 can be used for synthesis of PROTACs, such as PROTAC HPK1 Degrader-2 (HY-162544). HPK1-IN-47 can be used for research of HPK1-mediated diseases including cancer.
    HPK1-IN-47
  • HY-162922
    MAP4K4-IN-6
    Inhibitor
    MAP4K4-IN-6 (Compound 15f) is a MAP4K4 inhibitor (IC50: 80 nM). MAP4K4-IN-6 reduces the c-Jun phosphorylation. MAP4K4-IN-6 has neuroprotective effects. MAP4K4-IN-6 increases the viability of motor neurons. MAP4K4-IN-6 can be used for research of Amyotrophic lateral sclerosis (ALS).
    MAP4K4-IN-6
  • HY-145035
    HPK1-IN-9
    HPK1-IN-9 is potent inhibitor of HPK1. HPK1 is a serine/threonine protein kinase cloned from hematopoietic progenitor cells and belongs to the MAP4K family of mammalian Ste-20-related protein kinases. HPK1-IN-9 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 112) .
    HPK1-IN-9
  • HY-156509
    HPK1-IN-38
    Inhibitor
    HPK1-IN-38 (compound 15) is a MAP4K1/HPK1 inhibitor,can be used for HPK1 related disorders research.
    HPK1-IN-38
  • 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-145109
    HPK1-IN-20
    Inhibitor
    HPK1-IN-20 (Compound 106) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor.
    HPK1-IN-20
  • HY-173006
    AZ3246
    Inhibitor
    AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-volume, low-clearance antitumor compound.
    AZ3246
  • 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-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
  • 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

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