DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity[1].
DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM[1].DRB18 (5 and 10 μM; 72 hours) causes cell cycle arrest in the G1/S phase transition[1].DRB18 (5 and 10 μM; 72 hours) increases ROS levels in A549 cells[1].DRB18 (5 and 10 μM; 72 hours) reduces expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner[1].
DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%[1].
[1]. Shriwas P, Roberts D, Li Y, et al. A small-molecule pan-class I glucose transporter inhibitor reduces cancer cell proliferation in vitro and tumor growth in vivo by targeting glucose-based metabolism. Cancer Metab. 2021;9(1):14. Published 2021 Mar 26.