ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 5 μM).
CAS:1049738-54-6
分子式:C14H16N2O3S.HCl
分子量:328.8
纯度:98%
存储:Store at -20°C
Background:
ERK inhibitor is a cell-permeable inhibitor that binds ERK2 near its docking domain (KD = 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.