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DRB18 is a pan-inhibitor of glucose transporters (Gluts).1 It inhibits glucose uptake in HEK293 cells expressing Glut1, Glut2, Glut3, or Glut4 (IC50s = 2.6, 8.8, 4.5, and 0.9 µM, respectively) and in A549 and H1299 non-small cell lung cancer (NSCLC) cells (IC50s = 2.5 and 1.9 µM, respectively). DRB18 (10 µM) decreases the oxygen consumption rate (OCR) in a time-dependent manner, induces cell cycle arrest at the G1/S phase, and increases the levels of reactive oxygen species (ROS) in A549 cells. It decreases tumor volume and weight in an A549 mouse xenograft model when administered at a dose of 10 mg/kg.
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1. A small-