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 (67):

Cat. No. Product Name Effect Purity
  • 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-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[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 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)[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-163496
    HPK1-IN-45 Inhibitor
    HPK1-IN-45 (Compound 3) is a HPK1 inhibitor, with an IC50 of 0.3 nM. HPK1-IN-45 inhibits SLP-76 phosphorylation (IC50 = 57.52 nM) and IL-2 release (IC50 = 38 nM). HPK1-IN-45 can be used for the research of cancer[1].
  • HY-163495
    HPK1-IN-44 Inhibitor
    HPK1-IN-44 (Compound 1) is an inhibitor of HPK1 (IC50=0.1 nM (40 μM ATP))[1].
  • 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[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 immunoresearch tool compound[1].
  • 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.
  • 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-153553
    HPK1 antagonist-1 Antagonist
    HPK1 antagonist-1 (I-792) is an Hpk1 antagonist that can be used in the study of cancer and immune disease[1].
  • HY-160218
    HPK1-IN-42 Inhibitor
    HPK1-IN-42 (compound 185) ia a HPK1 inhibitor with the IC50 50 of 0.24 nM[1].
  • HY-153362
    HPK1-IN-34 Inhibitor
    HPK1-IN-34 (Compound 143) is a Hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <100 nM[1]. HPK1-IN-34 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
  • 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-163372
    PROTAC HPK1 Degrader-1 Degrader
    PROTAC HPK1 Degrader-1 (Compound B1) is a potent HPK1 degrader with DC50 value of 1.8 nM. PROTAC HPK1 Degrader-1 inhibits phosphorylation of the SLP76 protein with IC50 value of 496.1 nM. PROTAC HPK1 Degrader-1 is a bona fide HPK1-PROTAC degrader, which provided a potential tool for further HPK1 investigation in TCR signaling[1].
  • HY-15434A
    NG25 trihydrochloride Inhibitor
    NG25 trihydrochloride is a dual TAK1 and MAP4K2 inhibitor (IC50: 149 nM and 21.7 nM respectively). NG25 sensitizes the breast cancer cells to Doxorubicin (HY-15142A), and enhances apoptosis. NG25 trihydrochloride can be used for research of various cancers[1][2].
  • 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-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 immunoresearch[1].