DRB18 是一种有效的葡萄糖转运蛋白 (GLUT) 泛抑制剂。DRB18 通过改变葡萄糖相关途径中代谢产物的丰度来改变 A549 细胞中的能量相关代谢。DRB18 最终可导致细胞阻滞在 G1/S 期，增加氧化应激和坏死细胞死亡。DRB18 具有抗肿瘤活性。
| 生物活性 | DRB18 is a potent pan-classGLUTinhibitor. 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]. |
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体外研究
(In Vitro) | 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].
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 IC50s 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. |
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体内研究
(In Vivo) | DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(130.59 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.6118 mL | 13.0589 mL | 26.1178 mL | | 5 mM | 0.5224 mL | 2.6118 mL | 5.2236 mL | | 10 mM | 0.2612 mL | 1.3059 mL | 2.6118 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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