A 484954

A 484954 is a selective inhibitor of eEF2K with IC50 value of 0.28 μM [1].

Eukaryotic elongation factor-2 kinase (eEF2K) is a calcium/calmodulin-dependent protein kinase and regulates protein synthesis. It phosphorylates eEF2 and inhibits the activity of eEF2 [1].

A 484954 is a selective eEF2K inhibitor. A 484954 inhibited eEF2K and the phosphorylation of eEF2. While, it didn’t inhibit cancer cell growth. In enzymatic assay, the IC50 value of A-484954 was increased in an ATP-dependent way but not affected by the concentrations of calmodulin. In H1299 cells, A 484954 inhibited the phosphorylation of eEF2 but didn’t affect the protein level of eEF2. In PC3 cells, A 484954 (10 μM) inhibited peEF2 by 50% and the inhibition reached the maximum level at 100 μM. While A 484954 didn’t inhibit cell proliferation. In PC3 cells, NH125 induced eEF2 phosphorylation, while A 484954 had little effect on peEF2 induced by NH125 [1].

Reference:
[1].  Chen Z, Gopalakrishnan SM, Bui MH, et al. 1-Benzyl-3-cetyl-2-methylimidazolium iodide (NH125) induces phosphorylation of eukaryotic elongation factor-2 (eEF2): a cautionary note on the anticancer mechanism of an eEF2 kinase inhibitor. J Biol Chem, 2011, 286(51): 43951-43958.