A-484954

CAS号:142557-61-7
英文名:7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide
中文名:A-484954
CBNumber:CB02621577
分子式:C13H15N5O3
分子量:289.29
MOL File:142557-61-7.mol

A-484954化学性质

安全信息

A-484954性质、用途与生产工艺

简介 A-484954 是一种 ATP 竞争性的真核延伸因子 2 激酶 (eEF-2K；IC50 = 420 nM) 抑制剂。当以 75 μM 的浓度使用时，它可降低 PC3、HeLa、H460、H1299 和 MDA-MB-231癌细胞中的 eEF-2K自磷酸化。
生物活性 A-484954 是真核延长因子 2 (eEF2) 的高度选择性抑制剂，其 IC50 值为 280 nM。
靶点

IC50: 280 nM (eEF2).
体外研究

A-484954 is a highly selective eEF2K inhibitor with an IC ₅₀ value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC ₅₀ value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin.
体内研究

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. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation.

A-484954上下游产品信息

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下游产品

A-484954 试剂级价格

A-484954生产厂家