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.