| Description | 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]. |
| In vitro | DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC 50 s varying from ~ 900 nM to ~ 9 μM [1]. DRB18 (5 and 10 μM; 72 hours) results in 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]. Cell Proliferation Assay Cell Line: GLUT1-4-expressed HEK293 cell lines [1] Concentration: 0-10 μM Incubation Time: 30 min Result: Reduced glucose uptake in these cell lines in a dose-dependent manner with IC 50 s varying from ~ 900 nM to ~ 9 μM. Cell Cycle Analysis Cell Line: A549 [1] Concentration: 5 and 10 μM Incubation Time: 72 hours Result: Caused cell cycle arrest in the G1/S phase transition. Western Blot Analysis Cell Line: A549 [1] Concentration: 5 and 10 μM Incubation Time: 72 hours Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. Western Blot Analysis Cell Line: A549 [1] Concentration: 5 and 10 μM Incubation Time: 72 hours Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. |
| In vivo | DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) significantly inhibits tumors volume by 44% and tumors weight by 43% [1]. Animal Model: Male NU/J nude mice (3-4 weeks; tumor cell-injected) [1] Dosage: 10 mg/kg Administration: IP; thrice a week for 5 weeks Result: The tumors were 44% smaller by volume and 43% smaller by weight, also showed DRB18 decreased expression of GLUT1-4 (Fig. 5f) and reduced proliferative capacity within the xenografted tumor. |
| molecular weight | 382.88 |
| Molecular formula | C22H23ClN2O2 |
| CAS | 2863686-81-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (117.5 mM), Sonication and heating to 60℃ are recommended. |
| References | 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. |