Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor ( IC 50 =9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer . Takinib is also a P. falciparum protein kinase 9 ( Pf PK9) inhibitor (K D(app) of 0.46 μM).
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