DRB18

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

DRB18 

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。

DRB18

DRB18 Chemical Structure

规格 价格 是否有货
5 mg ￥2900 询问价格 & 货期
10 mg ￥4600 询问价格 & 货期
25 mg ￥9200 询问价格 & 货期
50 mg ￥14800 询问价格 & 货期

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生物活性

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].

IC50 & Target

GLUT[1]
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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

382.88

Formula

C22H23ClN2O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

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