| WZB117glucose transporter 1 (Glut1) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.79%
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| Cas No. | 1223397-11-2 | SDF | Download SDF |
| Synonyms | Glucose Transporter Inhibitor IV | ||
| 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 | ||
| Formula | C20H13FO6 | M.Wt | 368.3 |
| Solubility | ≥18.4mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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).
