ERK Inhibitor

Description

ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (K_D = 5 μM). This prevents its interaction with protein substrates without inhibiting catalytic activity. ERK inhibitor blocks ERK-specific phosphorylation of ribosomal S6 kinase-1 and ternary complex factor Elk-1 but does not affect ERK1/2 phosphorylation by MEK1/2. Presumably through its effects on ERK, ERK inhibitor completely prevents proliferation of HeLa cells (IC₅₀ = 15-20 μM), A549 lung carcinoma cells (IC₅₀ = 25 μM), Sum-159 estrogen receptor-negative breast cancer cells and HT1080 fibrosarcoma cells.

General Description

A cell-permeable and reversible thiazolidinedione compound that displays anti-proliferative properties (IC₅₀ ≤ 25 μM in HeLa, A549, and SUM-159 tumor cells). Preferentially binds to ERK2 with a K_D of ~5 μM and prevents its interaction with protein substrates. Shown to block ERK-mediated phosphorylation of ribosomal S6 kinase-1 (RSK-1) and ternary complex factor Elk-1 in HeLa cells, while exhibiting little effect on ERK1/2 phosphorylation by MEK1/2.

Biochem/physiol Actions

Primary TargetERK