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:

Cat. No. Product Name Effect Purity
  • HY-103490
    Takinib
    		Inhibitor 99.31%
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM).
  • HY-12686
    5Z-7-Oxozeaenol
    		Inhibitor 99.60%
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
  • HY-18938
    Selonsertib
    		Inhibitor 98.99%
    Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.
  • HY-112136
    TAO Kinase inhibitor 1
    		Inhibitor 99.46%
    TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
  • HY-12947
    GNE-3511
    		Inhibitor 99.85%
    GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.
  • 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.
  • 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.
  • HY-N1140
    Torilin
    		Inhibitor
    Torilin is a sesquiterpene with antimicrobial, anticancer, and anti-inflammatory properties. Torilin inhibits LPS-induced NO release, as well as inhibiting iNOS, PGE2, COX-2, NF-α, IL-1β, IL-6, and GM-CSF. Torilin suppresses NF-kB and AP-1 translocation, inhibits TAK1 kinase activation. Subsequently results suppression of MAPK-mediated JNK, p38, ERK1/2, and AP-1 (ATF-2 and c-jun) activation and IKK-mediated I-κBα degradation, p65/p50 activation, and translocation.
  • HY-32018
    Cot inhibitor-2
    		Inhibitor 99.22%
    Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
  • HY-100844
    GS-444217
    		Inhibitor 99.67%
    GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 nM.
  • 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-136848
    SM1-71
    		Inhibitor
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines.
  • HY-12358
    Tpl2 Kinase Inhibitor 1
    		Inhibitor 99.22%
    Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC50=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers.
  • HY-132172
    TAK1-IN-2
    		Inhibitor 98.22%
    TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM.
  • HY-19566
    NQDI-1
    		Inhibitor 98.03%
    NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a Ki of 500 nM and an IC50 of 3 μM.
  • HY-120823
    PF-05381941
    		Inhibitor 99.75%
    PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.
  • HY-32015
    Cot inhibitor-1
    		Inhibitor 98.06%
    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.
  • HY-124953
    7,3',4'-Trihydroxyisoflavone
    		Inhibitor 99.98%
    7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities.
  • HY-131969
    ASK1-IN-2
    		Inhibitor 98.49%
    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.
  • HY-114331
    DLK-IN-1
    		Inhibitor 99.41%
    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.
Cat. No. Product Name / Synonyms Application Reactivity
MAP3K Isoform Comparison

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