Takinib (EDHS-206) is a potent, selective TAK1 inhibitor with IC50 of 9.5 nM, selectively induces apoptosis following TNF-a stimulation.
Takinib weakly inhibits IRAK4, IRAK1, GCK, CLK2, and MINK1 with IC50 of 120-430 nM against the MRC Dundee kinase panel.
Takinib does not inhibit any of the MAP2Ks or MAP3Ks family members.
Takinib inhibits phosphorylation of IKK, MAPK 8/9, and c-Jun, induces apoptosis in RA fibroblast-like synoviocytes and reduces IL-6 secretion, induces TNF-α-dependent cell death in rheumatoid arthritis and breast cancer cells.
