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A 484954
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
A 484954图片
CAS NO:142557-61-7
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议

产品介绍
A 484954 是一种高选择性真核延伸因子-2 (eEF2) 抑制剂,IC50 为 280 nM。
Cas No.142557-61-7
化学名7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide
Canonical SMILESO=C(N(CC)C1=O)N(C2=NC(N)=C(C(N)=O)C=C21)C3CC3
分子式C13H15N5O3
分子量289.29
溶解度<2.89mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.