7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide

Description

A-484954 is an ATP-competitive inhibitor of eukaryotic elongation factor-2 kinase (eEF-2K; IC₅₀ = 420 nM). It reduces eEF-2K autophosphorylation in PC3, HeLa, H460, H1299, and MDA-MB-231 cancer cells when used at a concentration of 75 μM.

Uses

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.

Uses

7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide,a pyrido[2,3-d]pyrimidin-2,4(1H,3H)-dione derivative with potential use as herbicide antidote.

Biochem/physiol Actions

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.

storage

Store at +4°C