AMG-548, an orally active and selective p38α inhibitor ( K i =0.5 nM), shows slightly selective over p38β ( K i =36 nM) and >1000 fold selective against p38γ and p38δ . AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα ( IC 50 =3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
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