TAK1

TAK1/MAP4K2 inhibitor 1 is a potent dual inhibitor targeting transforming growth factor β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), exhibiting IC₅₀ values of 41.1 nM and 18.2 nM, respectively.

NG25, a TAK1 inhibitor, inhibited the activation of IKK by TLR7 and TLR9 agonists and prevented the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells.

Takinib is a selective TAK1 inhibitor that induces apoptosis following TNF-α stimulation in cell models of rheumatoid arthritis and metastatic breast cancer.

HS-243 is an inhibitor of transforming growth factor-?beta kinase. HS-243 can be used in treatment of cancer, malaria, inflammatory and other TAK1-?mediated diseases.

HS-276 is an orally bioavailable, potent, and highly selective inhibitor of transforming growth factor-β–activated kinase 1 (TAK1), with a Kᵢ of 2.5 nM. It exhibits strong inhibition of TAK1 and moderate activity against a panel of other kinases, including CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with respective IC₅₀ values ranging from 8.25 to 5585 nM. HS-276 is a valuable tool for investigating TAK1-mediated signaling pathways and holds therapeutic potential for inflammatory conditions such as rheumatoid arthritis (RA).

5Z-7-Oxozeaenol is a selective and irreversible inhibitor of TAK1, exhibiting an IC50 of 8 nM. This compound also inhibits VEGF-R2 with an IC50 of 52 nM, demonstrating potential applications in anti-protozoan research and studies related to inflammation and tumorigenesis. Its unique mechanism of action makes it a valuable tool for exploring signaling pathways associated with cellular stress responses and vascular biology.

SM1-71 is a potent TAK1 inhibitor exhibiting a Ki value of 160 nM. It targets multiple kinases, including MKNK2, MAP2K1/2/3/4/6/7, and GSK3A/B, among others, providing a broad scope of biological activity. This compound has demonstrated the ability to inhibit the proliferation of various cancer cell lines, making it a valuable tool for cancer research and therapeutic development.

Triptriolide is a TAK1 inhibitor that plays a pivotal role in regulating apoptosis in mouse podocytes. It enhances cell survival and protects podocyte function by modulating the Bcl-2 family proteins and inhibiting Caspase-3 activity. Additionally, Triptriolide activates the TAK1-NF-κB signaling pathway, leading to the upregulation of podocin. This reagent is relevant for studies focusing on kidney health and podocyte resilience under stress conditions.

(R)-STU104 is a selective inhibitor of the TAK1-MKK3 protein-protein interaction, demonstrating potent activity with IC50 values of 0.58 μM for TNF-α and 4.0 μM for MKK3 phosphorylation. By binding to MKK3, (R)-STU104 effectively disrupts the TAK1-mediated phosphorylation of MKK3, subsequently inhibiting the TAK1/MKK3/p38/MnK1/MK2/eIF4E signaling pathway. This compound is a valuable tool for investigating the molecular mechanisms underlying ulcerative colitis and related inflammatory conditions.

PF-05381941 is a potent dual inhibitor of TAK1 and p38α, exhibiting IC50 values of 156 nM and 186 nM, respectively. This compound effectively modulates the MAPK signaling pathway, making it a valuable tool for investigating cellular responses to stress and inflammation. PF-05381941 is commonly utilized in research focused on cancer, autoimmune diseases, and other pathological conditions linked to dysregulated kinase activity.