Figure 1
From: Econazole nitrate inhibits PI3K activity and promotes apoptosis in lung cancer cells
Putative PI3Kα inhibitors suppress lung cancer cell line viability. (A) Eight candidate PI3Kα inhibitors decreased the viability of H661 lung cancer cells with discrepant cytotoxicity at different concentrations. (B) Econazole (2.5, 5, 10, 20, or 40 μM) inhibited the viability of four NSCLC cell lines (H661, A549, H520 and SK-SEM-1) in a dose-dependent manner, but has little effect on BEAS-2B cells. The cells were treated with econazole for 24 hours. (C) The structure of econazole. (D) The predicted conformation of econazole in complex with PI3Kα (PDB ID: 4JPS). PI3Kα is depicted as a molecular surface representation colored by atom type. Econazole is rendered as sticks colored by atom type. Intermolecular interacting atoms and residues are labeled. The cyan and wheat dashed lines indicate a hydrogen bond and a halogen bond, respectively. This figure was created using the web-based visualizer iview. (E) The 24-hour cytotoxicity of econazole and two known PI3K inhibitors (PI3Kα-selective inhibitor BLY719 and pan-PI3K inhibitor BKM120) in H661 cells.
