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Merck
CN

SML0861

Sigma-Aldrich

A-484954

≥98% (HPLC)

Synonym(s):

7-Amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxo-pyrido[2,3-d]pyrimidine-6-carboxamideddd, A484954

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About This Item

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

Key Documents

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Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 3 mg/mL, clear (warmed)

storage temp.

2-8°C

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

Application

A-484954 has been used a selective and potent inhibitor to inhibit eEF2K (eukaryotic elongation factor 2 kinase), in order to check the enhancement of synaptic transmission in the stratum radiatum of the hippocampal CA1 region. It has also been used as an eEF2K inhibitor to monitor real-time luminescence of U2OS Arntl::dLUC cells.

Biochem/physiol Actions

A-484954 is a potent, selective inhibitor of eukaryotic longation factor-2 kinase (eEF2K).
A-484954 is a potent, selective inhibitor of eukaryotic longation factor-2 kinase (eEF2K). Eukaryotic elongation factor-2, which is required for protein synthesis, is inactivated upon phosphorylation by eEF2K.

Features and Benefits

This compound is featured on the Ca/CaMKs page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Storage Class Code

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

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Certificates of Analysis (COA)

Lot/Batch Number
0000034467
0000034468
0000022494
113M4747V

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Potentiation of Schaffer-Collateral CA1 Synaptic Transmission by eEF2K and p38 MAPK Mediated Mechanisms
Weng W, et al.
Frontiers in Cellular Neuroscience, 10, 247-247 (2016)
Acid Suspends the Circadian Clock in Hypoxia through Inhibition of mTOR
Walton Z E, et al.
Cell (2018)
Kanzo Suzuki et al.
Cell reports, 37(5), 109918-109918 (2021-11-04)
Ketamine is a noncompetitive glutamatergic N-methyl-d-aspartate receptor (NMDAR) antagonist that exerts rapid antidepressant effects. Preclinical studies identify eukaryotic elongation factor 2 kinase (eEF2K) signaling as essential for the rapid antidepressant action of ketamine. Here, we combine genetic, electrophysiological, and pharmacological
Zandra E Walton et al.
Cell, 174(1), 72-87 (2018-06-05)
Recent reports indicate that hypoxia influences the circadian clock through the transcriptional activities of hypoxia-inducible factors (HIFs) at clock genes. Unexpectedly, we uncover a profound disruption of the circadian clock and diurnal transcriptome when hypoxic cells are permitted to acidify

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