Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 96.00 | |
5 mg | In stock | $ 239.00 | |
10 mg | In stock | $ 378.00 | |
25 mg | In stock | $ 763.00 | |
50 mg | In stock | $ 1,230.00 | |
100 mg | In stock | $ 1,650.00 | |
500 mg | In stock | $ 3,290.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 263.00 |
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) 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. |
In vivo | 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. |
Molecular Weight | 382.88 |
Formula | C22H23ClN2O2 |
CAS No. | 2863686-81-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (117.5 mM), Sonication and heating to 60℃ are recommended.
You can also refer to dose conversion for different animals. More
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DRB18 2863686-81-9 Metabolism transporter DRB 18 DRB-18 inhibitor inhibit