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-132172
    TAK1-IN-2
    		Inhibitor 98.75%
    TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM.
    TAK1-IN-2
  • HY-114332
    GNE-8505
    		Inhibitor 99.86%
    GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).
    GNE-8505
  • HY-115743
    TAK1-IN-3
    		Inhibitor 98.88%
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
    TAK1-IN-3
  • HY-32015
    Cot inhibitor-1
    		Inhibitor 98.45%
    Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
    Cot inhibitor-1
  • 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-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-119608
    GSK854
    		Inhibitor 98.40%
    GSK854 is a potent Inhibitor of Troponin I-Interacting Kinase (TNNI3K). GSK854 is a suitable lead for identifying new cardiac medicines and have been employed as in vivo tools in investigational studies aimed at defining the role of TNNI3K within heart failure.
    GSK854
  • 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-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-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-122642
    TAK1-IN-4
    		Inhibitor 99.47%
    TAK1-IN-4 (Compound 14) is a TAK1 inhibitor.
    TAK1-IN-4
  • 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-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-160939
    ASK1-IN-6
    		Inhibitor 98.13%
    ASK1-IN-6 (Compound 32) is a selective inhibitor for apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 25 nM. ASK1-IN-6 is blood brain barrier penetrate(rat Cl/Clu is 1.6/56 L/h/kg and Kp,uu is 0.46). ASK1-IN-6 exhibits anti-inflammatory avtivity and ameliorates the Alzheimer’s Disease in Tg4510 mouse model.
    ASK1-IN-6
  • HY-136849
    TL13-68
    		Inhibitor 98.88%
    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-117658
    GSK-114
    		Inhibitor 98.08%
    GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC50= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC50= 1 μM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue.
    GSK-114
  • 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-D0885D
    Phosphocreatine disodium hydrate
    		Activator 99.57%
    Phosphocreatine (disodium hydrate) is an organic compound found in vertebrate skeletal muscles. Phosphocreatine (disodium hydrate) enhances antioxidant activity, and activates the TAK1 pathway to protect the heart. Phosphocreatine (disodium hydrate) normalizing mitochondrial function and reducing oxidative stress via Akt mediated Nrf2/HO-1 pathway. Phosphocreatine (disodium hydrate) Phosphocreatine (disodium hydrate) provides renal protection by suppressing Apoptosis and ROS (Reactive Oxygen Species) generation through ERK mediated mediated Nrf-2/HO-1 pathway..
    Phosphocreatine disodium hydrate
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
MAP3K Isoform Comparison

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