2. Signaling Pathways
  3. MAPK/ERK Pathway
  4. MAP3K

MAP3K

MAP kinase kinase kinase, MEKK, MAPKKK

MAP3K

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MAP3Ks (Mitogen-activated protein kinase kinase kinases), the top components of MAPK cascades, provide specificity for stimulus-dependent activation of MAP2K-MAPK pathways through unique protein-protein interactions and phosphorylation of signaling effectors. The MAP3Ks are highly divergent in gene numbers and structure, including TAK1, ASK1, A-Raf and C-Raf.

MAPK system is a three-step sequential phosphorylation cascade which is composed of MAPK, MAP2K, and MAP3K. ERK, p38 MAPK, and JNK, which are known to be activated by mechanical stimuli, belong to the MAPK family. MAP3Ks function as “platforms to integrate MAPK signaling, and activation of multiple MAP3Ks provides the spatiotemporal regulation of the MAPK pathways, which induces a wide range of physiological responses required for determining cell fate, such as cytokine production, survival, differentiation and apoptosis”.

MAP3K Isoform Specific Products:

MAP3K Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-77251
    TAK1/MAP4K2 inhibitor 1
    		Inhibitor 99.90%
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
    TAK1/MAP4K2 inhibitor 1
  • HY-120823
    PF-05381941
    		Inhibitor 99.73%
    PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.
    PF-05381941
  • HY-131969
    ASK1-IN-2
    		Inhibitor 99.55%
    ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.
    ASK1-IN-2
  • HY-115743
    TAK1-IN-3
    		Inhibitor 98.88%
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
    TAK1-IN-3
  • HY-133554
    ASK1-IN-1
    		Inhibitor 99.80%
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM).
    ASK1-IN-1
  • HY-114331
    DLK-IN-1
    		Inhibitor 99.18%
    DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM. DLK-IN-1 retains excellent CNS penetration and is well tolerated following multiple days of dosing at concentrations that exceed those required for DLK inhibition in the brain. DLK-IN-1 has activity in a model of Alzheimer’s Disease.
    DLK-IN-1
  • HY-103258
    TC ASK 10
    		Inhibitor 99.84%
    TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC50 of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC50 of 0.51 μM).
    TC ASK 10
  • HY-122642
    TAK1-IN-4
    		Inhibitor 99.47%
    TAK1-IN-4 (Compound 14) is a TAK1 inhibitor.
    TAK1-IN-4
  • HY-12383
    Pelubiprofen
    		Inhibitor 99.27%
    Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC50 values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.
    Pelubiprofen
  • 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.
    NG25 trihydrochloride
  • HY-153761
    ASK1-IN-4
    		Inhibitor
    ASK1-IN-4 (Compound 17) is an ASK1 inhibitor (IC50=0.2 μM). ASK1-IN-4 interacts with ATP-binding site of ASK1.
    ASK1-IN-4
  • HY-153320
    AZ-TAK1
    		Inhibitor
    AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines.
    AZ-TAK1
  • HY-124152
    3,4-Dephostatin
    		Inhibitor
    3,4-Dephostatin (Methyl-3,4-dephostatin) is an inhibitor of protein-tyrosine phosphatase (PTPase). 3,4-Dephostatin accelerates nerve growth factor (NGF)-induced neurite formation in PC12h cells. 3,4-Dephostatin sustains the NGF-induced tyrosine phosphorylation of proteins, most prominently that of mitogen-activated protein (MAP) kinase. 3,4-Dephostatin also prolongs epidermal growth factor (EGF)-induced tyrosine phosphorylation and activation of MAP kinase.
    3,4-Dephostatin
  • HY-122232
    SW083688
    		Inhibitor
    SW083688 is a potent, highly selective TAOK2 (Thousand-And-One Kinase 2) inhibitor (IC50 values = 1.3 umol/L).
    SW083688
  • HY-155089
    IACS-52825
    		Inhibitor
    IACS-52825 is a potent and selective DLK inhibitor with Kd of 1.3 nM, useful for the study of chemotherapy-induced peripheral neuropathy.
    IACS-52825
  • HY-157871
    TAK1-IN-5
    		Inhibitor
    TAK1-IN-5 (Compound 26) is an inhibitor of the transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. TAK1-IN-5 can inhibit the growth of MPC-11 and H929 cells with a GI50 lower than 30 nM. TAK1-IN-5 can be used in the study of multiple myeloma .
    TAK1-IN-5
  • HY-152247
    DDO3711
    		Inhibitor
    DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research.
    DDO3711
  • HY-18938A
    Selonsertib hydrochloride
    		Inhibitor
    Selonsertib hydrochloride (GS-4997 hydrochloride) is an orally bioavailable enzyme inhibitor with potential anti-inflammatory, anti-tumor and anti-fibrotic activities. Selonsertib hydrochloride blocks ASK1 phosphorylation and activation by binding to the catalytic kinase domain. Selonsertib hydrochloride prevents the production of inflammatory cytokines and reduces the expression of genes associated with fibrosis. Selonsertib hydrochloride inhibits excessive apoptosis and limits cell proliferation.
    Selonsertib hydrochloride
  • HY-E70291
    N-Acetylgalactosaminyltransferase 4
    		Inhibitor
    N-Acetylgalactosaminyltransferase 4 (GALNT4) is a glycosyltransferase capable of inhibiting the activation of ASK1. By directly binding to ASK1, N-Acetylgalactosaminyltransferase 4 suppresses its N-terminal dimerization and subsequent phosphorylation, leading to robust inactivation of downstream JNK/p38 and NF-κB signals, and thereby improving the prognosis of liver surgery.
    N-Acetylgalactosaminyltransferase 4
  • HY-146729
    ASK1-IN-3
    		Inhibitor
    ASK1-IN-3 is a potent and selective ASK1 kinase inhibitor with IC50 of 33.8 nM, as well as inhibits several cell cycle regulating kinases. ASK1-IN-3 has strong HepG2 cancer cells apoptosis induction and potent cell cycle arrest activities.
    ASK1-IN-3
Cat. No. Product Name / Synonyms Application Reactivity
MAP3K Isoform Comparison

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