Takinib is a selective TAK1 inhibitor with IC50 of 9.5 nM, it can induce apoptosis in a TNF-α-dependent manner in rheumatoid arthritis (RA) and breast cancer models.

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

5Z-7-Oxozeaenol is a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.