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

MAP3K Inhibitor

MAP3K Isoform Comparison

MAP3K Inhibitors (32):

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-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.
  • 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.
  • 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 .
  • 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-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-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-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-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-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-132172
    TAK1-IN-2
    		Inhibitor 98.22%
    TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM.
  • 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-77251
    TAK1/MAP4K2 inhibitor 1
    		Inhibitor 99.58%
    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.
  • HY-115743
    TAK1-IN-3
    		Inhibitor 98.88%
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.