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MAP3K

MAP3K (Mitogen Activated Protein (MAP) kinase kinase kinase) is a serine/threonine-specific protein kinase that acts on MAP kinases and belongs to the upstream component of the MAPK signaling pathway.Most of the MAP3Ks are activated by GPCR, stress, or growth factors, and then regulate the next level of the MAP2K and cascade reactions, which ultimately affect cell proliferation, differentiation, apoptosis and stress, and are implicated in cancer, inflammation and neurodegenerative diseases.

PF-05381941
T360171474022-02-0
PF-05381941 is a selective and potent dual inhibitor of TAK1 and p38α with IC 50 =156 nM 186nM that inhibits the kinase activity of TAK1 by binding to its active site.
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TAK-756
T204351
TAK-756 is a TAK1 inhibitor that selectively targets IRAK1 4 and exhibits excellent intra-articular pharmacokinetic properties. TAK1 is a potential molecular target for osteoarthritis (OA) due to its complementary anti-catabolic and anti-inflammatory effects.
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KAI-11101
T204384
KAI-11101 is an inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. It effectively suppresses paclitaxel-induced cJun phosphorylation (IC50=95 nM), thereby inhibiting the activation of the MAPK pathway. KAI-11101 exhibits blood-brain barrier permeability, allowing for further exploration of its neuroprotective properties.
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PROTAC LZK-IN-1
T2043732763268-64-8
PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates 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. This compound is applicable in anticancer research.
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