| Description | WZB117 is a Glucose Transporter 1 (GLUT1) inhibitor. when IC50 of WZB117 approximate 10 μM, it inhibits lung cancer A549 cells and breast cancer MCF7 cells proliferation. |
| In vitro | WZB117 treats Cancer cell resulting in decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. And WZB117 inhibits glucose transport in human red blood cells. The declines in cyclin E2 as well as phosphorylated retinoblastoma and increases in ATP-sensing enzyme AMP-activated protein kinase (AMPK), lead to the cell-cycle arrest, senescence, and necrosis. |
| In vivo | WZB117每日通过腹腔注射给予裸鼠10 mg/kg，这些裸鼠被移植了人类A549肺癌细胞，结果显示肿瘤体积减少了70%。 |
| Cell experiments | Human non–small cell lung cancer (NSCLC) cell lines H1299 and A549 are treated with compound WZB117（10 μM） for 24 or 48 hours. |
| Animal experiments | Male NU/J nude mice were given intraperitoneal injection with WZB117 (10 mg/kg) daily for 10 weeks. |
| Target activity | GLUT1:10μM |
| molecular weight | 368.31 |
| Molecular formula | C20H13FO6 |
| CAS | 1223397-11-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 36.8 mg/mL (100 mM) Ethanol: 36.8 mg/mL (100 mM) |
| References | 1. Liu Y, et al. Mol Cancer Ther. 2012, 11(8):1672-1682. 2. Chen J, Wu D, Dong Z, et al. The expression and role of glycolysis-associated molecules in infantile hemangioma[J]. Life Sciences. 2020, 259: 118215. |
| Citations | 1. Chen X, Zhao Y, He C, et al. Identification of a novel GLUT1 inhibitor with in vitro and in vivo anti-tumor activity. International Journal of Biological Macromolecules. 2022, 216: 768-778. 2. Chen J, Wu D, Dong Z, et al. The expression and role of glycolysis-associated molecules in infantile hemangioma. Life Sciences. 2020, 259: 118215. 3. Liu Y, Hou Y, Zhang F, et al.ENO1 deletion potentiates ferroptosis and decreases glycolysis in colorectal cancer cells via AKT/STAT3 signaling.Experimental and Therapeutic Medicine.2024, 27(4): 1-9. |