2. MAPK/ERK Pathway
  3. MAP4K

MAP4K

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 Related Products (90):

Cat. No. Product Name Effect Purity
  • 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.
  • 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 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[1][2].
  • 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)[1].
  • HY-100343
    GNE-495 Inhibitor 99.49%
    GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.
  • HY-172594
    HPK1-IN-57 Inhibitor
    HPK1-IN-57 (Compound 10c) is a hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.09 nM. HPK1-IN-57 inhibits the activity of HPK1 kinase, hindering the phosphorylation of the downstream adaptor protein SLP76 (IC50 is 33.74 nM) and effectively stimulating the secretion of the T cell activation marker IL-2 (EC50 is 84.24 nM). HPK1-IN-57 is promising for research of tumor immunotherapy[1].
  • 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)[1][2].
  • 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-clearance antitumor compound[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-159123
    KHK-6 Inhibitor
    KHK-6 is an inhibitor for serine/threonine kinase hematopoietic progenitor kinase 1 (HPK 1) with an IC50 of 20 nM. KHK-6 enhances CD3/CD28-induced cytokine production, enhances CD69, CD25 and HLA-DR markers on CD4+ and CD8+ T cells, and enhances T cell-mediated killing activity of SKOV3 and A549 cells[1].
  • HY-138569
    HPK1-IN-4 Inhibitor 99.42%
    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 99.70%
    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-162816
    PROTAC HPK1 Degrader-3
    PROTAC HPK1 Degrader-3 (compound C3) is an orally effective PROTAC targeting HPK1 (DC50=21.26 nM). HPK1 is a negative regulator of T cell receptors, which can lead to T cell dysfunction after abnormal activation. PROTAC HPK1 Degrader-3 can inhibit SLP76 and NF-κB signaling pathways and inhibit MAPK signal transduction, and has anticancer activity and immune activation. PROTAC HPK1 Degrader-3 has a certain oral bioavailability and can be combined with PD-L1 antibody therapy to achieve a tumor growth inhibition rate of 65.58%. PROTAC HPK1 Degrader-3 is composed of E3 ligase ligand Thalidomide (HY-14658; blue part), PROTAC linker tert-Butyl 3-oxoazetidine-1-carboxylate (HY-40146; black part), and target protein ligand HPK1-IN-51 (HY-162842; red part); the activity control of the target protein ligand can be HPK1 ligand 1 (HY-162841)[1].