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化學性質:
規格 | 5mg 10mg 25mg |
CAS | 122 |
別名 | Glucose Transporter Inhibitor IV |
化學名 | 3-hydroxy-benzoic acid, (3-fluoro-1,2-phenylene)ester |
分子式 | C20H13FO6 |
分子量 | 368.3 |
溶解度 | ≥ 18.4mg/mL in DMSO |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
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.
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原創作者:上海莼試生物技術有限公司
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開 戶 行:中國銀行山東省分行營業部
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