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Merck
CN

324516

Sigma-Aldrich

A-484954

≥98% (HPLC), powder, eEF2K inhibitor, Calbiochem®

别名:

eEF2K Inhibitor, A-484954, 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1,2,3,4-tetrahydropyrido[2,3-d]pyrimidine-6-carboxamide, Eukaryotic elongation factor-2 kinase inhibitor, A-484954

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关于此项目

经验公式（希尔记法）:
C13H15N5O3
化学文摘社编号:
142557-61-7
分子量:
289.29
MDL编号:
MFCD22683836
UNSPSC代码:
12352200
NACRES:
NA.77

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产品名称

eEF2K Inhibitor, A-484954, The eEF2K Inhibitor, A-484954, also referenced under CAS 142557-61-7, controls the biological activity of eEF2K Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

质量水平

100

方案

≥98% (HPLC)

表单

powder

制造商/商品名称

Calbiochem®

储存条件

OK to freeze
protect from light

颜色

off-white

溶解性

DMSO: 2.5 mg/mL, clear, colorless

运输

wet ice

储存温度

2-8°C

SMILES字符串

O=C(C1=C(N2C3CC3)N=C(N)C(C(N)=O)=C1)N(CC)C2=O

InChI

1S/C13H15N5O3/c1-2-17-12(20)8-5-7(10(15)19)9(14)16-11(8)18(13(17)21)6-3-4-6/h5-6H,2-4H2,1H3,(H2,14,16)(H2,15,19)

InChI key

HWODCHXORCTEGU-UHFFFAOYSA-N

相关类别

一般描述

A cell-permeable pyrido-pyrimidinedione derivative that acts as a highly potent and selective inhibitor of eukaryotic elongation factor-2 kinase (eEF2K) (IC50= 280 nM). Exhibits very little activity against a broad panel of serine/threonine and protein tyrosine kinases. Inhibits eEF2 phosphorylation in multiple cell lines tested without affecting the net eEF2 levels. At concentration where it inhibits eEF2K activity, it has no effect on the proliferation of cancer cell lines.

包装

Packaged under inert gas

制备说明

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Chen, Z., et al. 2011. J. Bio. Chem.286, 43951.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

分析证书(COA)

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Megha Jhanji et al.
Nature communications, 13(1), 3244-3244 (2022-06-11)
Serum tyrosine levels increase during aging, neurocognitive, metabolic, and cardiovascular disorders. However, calorie restriction (CR) and sleep lower serum tyrosine levels. We previously showed that tyrosine inhibits tyrosyl-tRNA synthetase (TyrRS)-mediated activation of poly-ADP-ribose polymerase 1 (PARP1). Here, we show that
Julie Pires Da Silva et al.
Cells, 9(2) (2020-02-16)
Many recent studies have demonstrated the involvement of endoplasmic reticulum (ER) stress in the development of cardiac diseases and have suggested that modulation of ER stress response could be cardioprotective. Previously, we demonstrated that the deacetylase Sirtuin 1 (SIRT1) attenuates
Sujata Jana et al.
Cancer cell, 41(5), 853-870 (2023-04-22)
We uncover a tumor-suppressive process in urothelium called transcriptional-translational conflict caused by deregulation of the central chromatin remodeling component ARID1A. Loss of Arid1a triggers an increase in a nexus of pro-proliferation transcripts, but a simultaneous inhibition of the eukaryotic elongation

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