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经验公式(希尔记法):
C13H15N5O3
化学文摘社编号:
分子量:
289.29
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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.
SMILES string
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
assay
≥98% (HPLC)
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
off-white
solubility
DMSO: 2.5 mg/mL, clear, colorless
shipped in
wet ice
Quality Level
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General description
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.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Chen, Z., et al. 2011. J. Bio. Chem.286, 43951.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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
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