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ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 µM).1 This prevents its interaction with protein substrates without inhibiting catalytic activity.1 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 MEK1/2.1 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.1
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1. Identification of novel extracellular signal-