2. Signalwege
  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
Art. -Nr. Produktname Wirkung Reinheit Chemical Structure
  • HY-117243
    GSK329
    		Inhibitor 99.60%
    GSK329 is a potent and selective diarylurea inhibitor of the cardiac-specific kinase TNNI3K. GSK329 exhibits positive cardioprotective outcomes in the model of ischemia/reperfusion cardiac injury.
    GSK329
  • 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-136849
    TL13-68
    		Inhibitor 98.31%
    TL13-68 is a biotin-tagged version of SM1-71, and it can be used to research the mechanism of SM1-71.
    TL13-68
  • HY-169949
    TAK-756
    		Inhibitor
    TAK-756 is a selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with a target pIC50 of 8.6. TAK-756 can inhibit TAK1 autophosphorylation and downstream NF-κB phosphorylation, suppress the production of inflammatory and catabolic factors such as MMP-3 and IL-6. TAK-756 exhibits anti-inflammatory effects in a rat joint inflammation model. TAK-756 can be used for the research of inflammatory joint disease, osteoarthritis.
    TAK-756
  • HY-16129
    CBP-501
    		Inhibitor 99.75%
    CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of cancer.
    CBP-501
  • 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-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-178726
    Cot-IN-4
    		Inhibitor
    Cot-IN-4 (compound 32) is a potent cancer osaka thyroid (COT) kinase inhibitor with an IC50 of 6 nM. Cot-IN-4 inhibits the phosphorylation of ERK (IC50: 60 nM) and inhibits TNFα release (IC50: 60 nM). Cot-IN-4 also inhibits the formation of the pro-inflammatory cytokine IL-1β (IC50: 0.2 μM) in Uric acid (HY-B2130)-stimulated macrophages. Cot-IN-4 can be used for the study of inflammatory diseases.
    Cot-IN-4
  • 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-16129A
    CBP-501 acetate
    		Inhibitor 99.75%
    CBP-501 acetate, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser216-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC50 values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 acetate is used for various types of cancer.
    CBP-501 acetate
  • HY-136807
    Tpl2-IN-I
    		Inhibitor
    Tpl2-IN-I functions as an inhibitor of the Tpl2 (tumour progression locus 2) kinase.
    Tpl2-IN-I
  • HY-170595
    PROTAC LZK degrader 1
    		Degrader
    PROTAC LZK degrader 1 (Compound 21A) is a PROTAC that targets the degradation of LZK (Leucine Zipper Kinase, encoded by MAP3K13). PROTAC LZK degrader 1 (10 μM) promotes the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. PROTAC LZK degrader 1 can be used in cancer research. PROTAC LZK degrader 1 consists of an E3 ligase ligand (blue part, HY-112078), a target protein ligand (red part, HY-170596), and a linker (black part, HY-W019543)[1].
    PROTAC LZK degrader 1
  • HY-P5522
    TriDAP
    		Activator
    TriDAP (L-Ala-γ-D-Glu-meso-diaminopimelic acid) is a NOD1 agonist with a Kd value of 34.5 μM. TriDAP enhances the binding of NOD1-RICK, promotes RICK phosphorylation, and activates the NF-κB, TAK1, MEK/ERK, p38 and interferon response pathways. TriDAP downregulates Runx2 via increasing ubiquitination and reduces trabecular bone parameters. TriDAP decreases IκBα levels and increases p65 levels. TriDAP induces the secretion of proinflammatory mediators IL-8 and prostaglandins, triggers tissue inflammation and innate immune activation, and inhibits SARS-CoV-2 replication in lung epithelial cells. TriDAP increases the RANKL/OPG ratio in mice, reduces bone mass and enhances osteoclast activity, and inhibits new bone formation by decreasing the mineralization deposition rate in mice. TriDAP can be used in research related to pulpitis, chronic ulcerative colitis, Crohn's disease and SARS-CoV-2 infection.
    TriDAP
  • 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-181662
    DLK-IN-2
    		Inhibitor
    DLK-IN-2 is a selective inhibitor of DLK and neuroprotective agent. DLK-IN-2 shows no significant inhibition against CYPs 3A4, 2D6 and 2C9. DLK-IN-2 inhibits acute axonal palmitoylation of DLK, blocks DLK-dependent pro-degenerative axon-to-soma retrograde signaling and suppresses c-Jun phosphorylation. DLK-IN-2 can be used for the mechanistic study of neurodegenerative diseases.
    DLK-IN-2
  • HY-172871
    Anti-inflammatory agent 102
    		Inhibitor
    Anti-inflammatory agent 102 (Compound 11a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 102 exerts its anti-inflammatory effect by blocking the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. Anti-inflammatory agent 102 has significant anti-inflammatory activity and can inhibit the release of NO, ROS, and inflammatory factors (such as IL-6, TNF-α, IL-1β). Anti-inflammatory agent 102 can be used in the study of inflammatory diseases such as ulcerative colitis (UC).
    Anti-inflammatory agent 102
Art. -Nr. Produktname / Synonyms Application Reactivity
MAP3K Isoform Comparison

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