化合物DRB18 T22317

Product Introduction
Bioactivity


英文名: DRB18

描述: 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].

体外活性: 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.

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (117.5 mM)


关键字: DRB 18 | DRB18 | DRB-18

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相关库: Anti-Cancer Metabolism Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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