324516

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.

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

Properties

• 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

Description

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable