MAP3K
MAP kinase kinase kinase, MEKK, MAPKKK
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
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MAP3K
(36)
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MAP3K7/
TAK1 (11)View all products
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MAP3K8/
COT/ (4)Tpl2 View all products
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MAP3K6/
ASK2 (1)View all products
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MAP3K5/
ASK1 (15)View all products
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MAP3K12/
DLK/ (2)Pref-1 View all products
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TNNI3K/
HH498 (1)View all products
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MAP3K13/
LZK (3)View all products
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MAP3K1
(1)
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NIK/
MAP3K14 (1)View all products
All Product Categories
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MAP3K Related Products (87)
Related Products (87)
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Antibodies (11)
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MAP3K Isoform Comparison
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GSK329
0 ImagesGSK329 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.
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PF-05381941
0 ImagesPF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively.
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TAK-756
0 ImagesCat. No.: HY-169949CAS No.: 3097983-41-7TAK-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.
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CBP-501
0 ImagesCat. No.: HY-16129CAS No.: 565434-85-7CBP-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.
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NG25 trihydrochloride
0 ImagesCat. No.: HY-15434ACAS No.: 2108554-00-1NG25 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.
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MAP3K14-IN-1
0 ImagesCat. No.: HY-124865CAS No.: 2113617-02-8MAP3K14-IN-1 (Compound 173) is a MAP3K14 (NIK kinase) inhibitor with an IC50 of 1.8 nM. MAP3K14-IN-1 inhibits the autophosphorylation of MAP3K14 kinase. MAP3K14-IN-1 reduces the level of phosphorylated IKKα in cancer cells. MAP3K14-IN-1 inhibits the proliferation of multiple myeloma cells. MAP3K14-IN-1 can be used in research related to multiple myeloma.
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ASK1-IN-4
0 ImagesCat. No.: HY-153761CAS No.: 1427538-26-8
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CS17919
0 ImagesCat. No.: HY-163752CAS No.: 2379346-41-3CS17919 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.
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SW-034538
0 ImagesCat. No.: HY-124059CAS No.: 412919-82-5SW-034538 is a TAO2 inhibitor, with an IC50 of 300 nM.
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AZ-TAK1
0 ImagesCat. No.: HY-153320CAS No.: 1413440-36-4AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines.
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Cot-IN-4
0 ImagesCat. No.: HY-178726CAS No.: 1984784-10-2Cot-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.
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3,4-Dephostatin
0 ImagesCat. No.: HY-124152CAS No.: 173043-84-0Synonyms: Methyl-3,4-dephostatin3,4-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.
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CBP-501 acetate
0 ImagesCat. No.: HY-16129APurity: 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.
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Tpl2-IN-I
0 ImagesCat. No.: HY-136807CAS No.: 915009-13-1Tpl2-IN-I functions as an inhibitor of the Tpl2 (tumour progression locus 2) kinase.
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PROTAC LZK degrader 1
0 ImagesCat. No.: HY-170595CAS No.: 2763268-64-8PROTAC LZK degrader 1 is an LZK (MAP3K13) PROTAC degrader. PROTAC LZK degrader 1 binds LZK with a Kd of 35 nM and recruits VHL E3 ubiquitin ligase to induce ubiquitin-proteasome dependent degradation of LZK in MAP3K13-amplified HNSCC cells. PROTAC LZK degrader 1 eliminates both kinase-dependent c-MYC stabilization and kinase-independent GOF p53 accumulation downstream of LZK, suppresses colony formation of LZK-amplified head and neck squamous cell carcinoma (HNSCC) cells. PROTAC LZK degrader 1 can be used for research on LZK-driven HNSCC.
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TriDAP
0 ImagesCat. No.: HY-P5522CAS No.: 877462-71-0Synonyms: L-Ala-γ-D-Glu-meso-diaminopimelic acidTriDAP (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.
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LZK-IN-1
0 ImagesCat. No.: HY-189202CAS No.: 2912371-82-3LZK-IN-1 is an orally active and selective LZK inhibitor with a Kd of 2.7 nM. LZK-IN-1 disrupts the LZK-AKT protein-protein interaction, blocks AKT autophosphorylation, and reduces the activation of the downstream JNK pathway. LZK-IN-1 inhibits the proliferation of cancer cells with MAP3K13 amplification and reduces in vivo tumor growth in xenograft mouse models. LZK-IN-1 can be used for the study of esophageal squamous cell carcinoma and head and neck squamous cell carcinoma with MAP3K13 amplification.
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TAK1-IN-5
0 ImagesCat. No.: HY-157871TAK1-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 .
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DDO3711
0 ImagesCat. No.: HY-152247CAS No.: 2673364-10-6DDO3711, 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.
