A-484954 是一种高度特异性的真核延伸因子-2 抑制剂，其IC50值为 280 nM。
产品描述
A 484954 is a highly specific eukaryotic elongation factor-2 (eEF2, IC50: 280 nM) inhibitor.
体外活性
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].
体内活性
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].
Cas No.
142557-61-7
分子式
C13H15N5O3
分子量
289.29
别名
A 484954
储存和溶解度
H2O:Insoluble
DMSO:20 mg/mL (69.13 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
