1. MAPK/ERK Pathway
  2. MAP4K

MAP4K

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 Related Products (43):

Cat. No. Product Name Effect Purity
  • HY-135892
    GNE-1858 Inhibitor 99.36%
    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[1].
  • HY-111754
    DMX-5804 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[1].
  • HY-100830
    NCB-0846 Inhibitor 99.61%
    NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.
  • HY-138568
    HPK1-IN-3 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)[1].
  • HY-100343
    GNE-495 Inhibitor 99.40%
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
  • HY-152257
    HPK1-IN-31
    HPK1-IN-31 (compound 5i) is an orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.8 nM. HPK1-IN-31 has anti-tumour activity and has great potential for immunotherapy[1].
  • 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[1].
  • 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.
  • HY-138569
    HPK1-IN-4 Inhibitor 99.09%
    HPK1-IN-4 (comp 22) is a HPK1 (MAPK41) inhibitor (IC50 of 0.061 nM) as preclinical immunotherapy tool compound[1].
  • 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-145041
    HPK1-IN-15 Inhibitor
    HPK1-IN-15 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-15 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2018049200A1, compound 50)[1].
  • HY-144073
    HPK1-IN-21 Inhibitor
    HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active[1].
  • HY-145042
    HPK1-IN-16 Inhibitor
    HPK1-IN-16 is a potent and selective inhibitor of HPK1. Hematopoietic progenitor kinase 1 (HPKl) originally cloned from hematopoietic progenitor cells is a member of MAP kinase kinase kinase kinases (MAP4Ks) family. HPK1-IN-16 is useful in researching, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer (extracted from patent WO2019051199A1, compound 39)[1].
  • HY-132926
    HPK1-IN-8 Inhibitor 98.56%
    HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.
  • 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.
  • HY-144088
    ZYF0033 Inhibitor
    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[1].
  • HY-145039
    HPK1-IN-13 Inhibitor
    HPK1-IN-13 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-13 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 64) [1].
  • HY-145038
    HPK1-IN-12 Inhibitor
    HPK1-IN-12 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-12 has the potential for the research of HPK1 related diseases (extracted from patent WO2021213317A1, compound 85) [1].
  • HY-123714
    TL4-12 Inhibitor
    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 drug resistance in multiple myeloma (MM)[1].
  • HY-143868
    HPK1-IN-27 Inhibitor
    HPK1-IN-27 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-27 has the potential for the research of cancer diseases (extracted from patent WO2019016071A1, compound 38)[1].