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Sigma-Aldrich

A-484954

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

Synonym(s):

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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About This Item

Empirical Formula (Hill Notation):
C13H15N5O3
CAS Number:
142557-61-7
Molecular Weight:
289.29
MDL number:
MFCD22683836
UNSPSC Code:
12352200
NACRES:
NA.77

product name

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.

Quality Level

100

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

storage temp.

2-8°C

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

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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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
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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