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。
货号:ajcx37868
CAS:N/A
分子式:C22H23ClN2O2
分子量：382.88
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) inhibits tumors volume by 44% and tumors weight by 43%[1].

[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.