WZB117glucose transporter 1 (Glut1) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.79%
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Chemical structure
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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).
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硝酸根从根向地上部茎的长距离运输过程中首先要进行木质部的装载。台湾科学家发现NRT1.5是一个低亲和且依赖于pH的双向转运蛋白,位于质膜并在靠近木质部的中柱鞘细胞中表达,对于硝酸根在木质部的装载具有重要作用。
所以NRT1.5是双向性的转运蛋白
另外在八版生理248页第二段,近端小管后半段氯离子通过氯离子碳酸氢根交换体被重吸收,此时小管液中氯离子浓度大于周围组织液氯离子浓度,所以也有细胞旁途径顺浓度被动重吸收,然而资料上的总结和题目里都是说氯离子在近端小管的重吸收为被动重吸收,感觉有些糊涂。希望来个大神指点一二。
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