| CAS NO: | 1223397-11-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Storage | Store at -20°C |
| M.Wt | 368.3 |
| Cas No. | 1223397-11-2 |
| Formula | C20H13FO6 |
| Synonyms | Glucose Transporter Inhibitor IV |
| Solubility | insoluble in H2O; ≥18.4 mg/mL in DMSO; ≥42.6 mg/mL in EtOH |
| Chemical Name | 3-hydroxy-benzoic acid, (3-fluoro-1,2-phenylene)ester |
| Canonical SMILES | OC1=CC=CC(C(OC2=CC=CC(F)=C2OC(C3=CC(O)=CC=C3)=O)=O)=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
IC50: ~0.6 μM for blocking glucose transport in diverse cancer cells
WZB117 is a glucose transporter 1 (Glut1) inhibitor.
Glucose transporter 1 (GLUT1), a uniporter protein that in humans is encoded by the SLC2A1 gene, facilitates the transport of glucose across the plasma membranes of mammalian cells. GLUT1 is responsible for the low level of basal glucose uptake to maintain respiration. Expression levels of GLUT1 in cell membranes are increased by reduced glucose levels and decreased by increased glucose.
In vitro: Previous study found that WZB117 could inhibit glucose transport in human red blood cells expressing Glut1 as their sole glucose transporter. Moreover, cancer cell treatment with WZB117 resulted in decreased levels of Glut1 protein, intracellular ATP, as well as glycolytic enzymes. All these changes were followed by increase in ATP-sensing enzyme AMP-activated protein kinase and declined in cyclin E2 as well as phosphorylated retinoblastoma, leading to cell-cycle arrest, senescence, and necrosis [1].
In vivo: Animal study showed that the daily ip injection of WZB117 at 10 mg/kg led to a more than 70% reduction in the size of human lung cancer of A549 cell origin [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Liu, Y. ,Cao, Y.,Zhang, W., et al. A small-molecule inhibitor of glucose transporter 1 downregulates glycolysis, induces cell-cycle arrest, and inhibits cancer cell growth in vitro and in vivo. Mol. Cancer Ther. 11(8), 1672-1682 (2012).
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