A-484954 (A 484954) is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.

eEF2:280 nM

A-484954 is a selective eEF2K inhibitor and little activity against a wide panel of serine/threonine and tyrosine kinases. In the enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin [1].

Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation [2]. A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery [3].