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-163752
    CS17919
    		Inhibitor
    CS17919 is a potent, selective and orally active ASK1 inhibitor with an IC50 of 22.52 nM. CS17919 shows anti-inflammatory and antifibrotic effects. CS17919 can be used for the study of metabolic-related kidney and liver diseases.
    CS17919
  • HY-124059
    SW-034538
    		Inhibitor
    SW-034538 is a TAO2 inhibitor, with an IC50 of 300 nM.
    SW-034538
  • 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-170484
    KAI-11101
    		Inhibitor
    KAI-11101 is the inhibitor for dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. KAI-11101 inhibits Paclitaxel (HY-B0015)-induced cJun phosphorylation (IC50=95 nM) and thus inhibits the activation of MAPK pathway. KAI-11101 is blood brain barrier penetrable and can be further investigated for its neuroprotective property.
    KAI-11101
  • 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-169153
    Cot inhibitor-3
    		Inhibitor
    Cot inhibitor-3 (Compound 33) is a potent and selective cancer osaka thyroid (COT) kinase inhibitor, with an IC50 of 4 nM. Cot inhibitor-3 can be used to prevent inflammation-driven lameness.
    Cot inhibitor-3
  • 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
  • HY-110262
    MSC 2032964A
    		Inhibitor
    MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation.
    MSC 2032964A
  • HY-N2037AS1
    Higenamine-d4-1 hydrochloride
    Higenamine-d4-1 (Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
    Higenamine-d<sub>4</sub>-1 hydrochloride
  • HY-N0156R
    Oleanolic acid (Standard)
    Oleanolic acid (Standard) is the analytical standard of Oleanolic acid. This product is intended for research and analytical applications. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
    Oleanolic acid (Standard)
  • HY-N2037AR
    Higenamine (hydrochloride) (Standard)
    Higenamine (hydrochloride) (Standard) is the analytical standard of Higenamine (hydrochloride). This product is intended for research and analytical applications. Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases.
    Higenamine (hydrochloride) (Standard)
  • HY-18297
    ASK1-IN-5
    		Inhibitor
    ASK1-IN-5 (S-99) is an inhibitor of apoptosis signal-regulated kinase 1 (ASK1) and is useful in the study of autoimmune and neurodegenerative diseases.
    ASK1-IN-5
  • HY-161283
    JT21-25
    		Inhibitor
    JT21-25 (compound 9h) is a potent and selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with IC50 of 5.1 nM.
    JT21-25
  • HY-N15315
    Triptriolide
    		Activator
    Triptriolide inhibits Puromycin aminonucleoside PAN (HY-15695)-induced apoptosis in mouse podocytes through regulation of Bcl-2 family proteins and inhibition of Caspase-3. Triptriolide promotes the cell survival, protects and restores the podocyte function through activation of TAK1-NF-κB signaling pathway and upregulation of podocin.
    Triptriolide
Cat. No. Product Name / Synonyms Application Reactivity
MAP3K Isoform Comparison

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