Biological Activity
AMG-548 is a potent, oral and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γand p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) [1]. AMG-548 inhibits Wnt signaling by direcly inhibing Casein kinase 1 isoforms δ and ε[2].
In Vitro
No in vitro data are provided in the current product source. Contact us for further information.
In Vivo
AMG-548 has rat F of 62% and dog F of 47%. The t1/2 is 4.6 hours in rats and 7.3 hours in dogs[1].
References & source
1. Verkaar F, et al. Chem Biol. 2011 Apr 22;18(4):485-94.
2. Lee MR, et al. Curr Med Chem. 2005;12(25):2979-94.
3. Dominguez C, et al. Curr Opin Drug Discov Devel. 2005 Jul;8(4):421-30.
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.