DRB18 is a highly effective pan-class inhibitor of glucose transporter proteins (GLUT). It significantly modulates energy-related metabolism in A549 cells by inducing alterations in the abundance of metabolites associated with glucose-related pathways. DRB18 exerts its effects by promoting G1/S phase arrest, increasing oxidative stress, and prompting necrotic cell death, ultimately displaying notable anti-tumor activity [1].

DRB18 (0-10 μM; 30 min) demonstrably decreases glucose absorption in a dose-dependent manner within HEK293 cells expressing GLUT1-4, with inhibitory concentration (IC50) values ranging approximately from 900 nM to 9 μM [1]. Additionally, at concentrations of 5 and 10 μM over 72 hours, DRB18 induces cell cycle arrest at the G1/S phase transition and elevates reactive oxygen species (ROS) levels in A549 cells [1]. Concurrently, it diminishes the expression of the glycosylated forms of GLUT1 and GLUT2-4 in A549 cells, following a dose-responsive relationship [1]. These findings were derived from cell proliferation assays on HEK293 cell lines, and cell cycle as well as western blot analyses on A549 cell lines, underscoring DRB18's multifaceted biochemical impacts.

DRB18 administered at a dosage of 10 mg/kg intraperitoneally (IP) three times a week for five weeks significantly reduced tumor volume and weight by 44% and 43%, respectively, in male NU/J nude mice aged 3-4 weeks with injected tumor cells. This treatment also resulted in decreased expression of GLUT1-4 and reduced proliferative capacity within the xenografted tumor.