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In vitro: WZB117 inhibits glucose transport in human red blood cells. Cancer cell treatment with WZB117 leads to decreases in levels of Glut1 protein, intracellular ATP, and glycolytic enzymes. All these changes are followed by increase in ATP-sensing enzyme AMP-activated protein kinase (AMPK) and declines in cyclin E2 as well as phosphorylated retinoblastoma, resulting in cell-cycle arrest, senescence, and necrosis.
In vivo: Daily intraperitoneal injection of WZB117 at 10mg/kg resultes in 70% reduction in tumor volume of human A549 lung cancer grafted on nude mice.
| Cell Experiment | |
|---|---|
| Cell lines | Human non–small cell lung cancer (NSCLC) cell |
| Preparation method | Cells were treated with compound WZB117 for 24 or 48 hours. WZB117 (10 μmol/L) was used in the experiments unless otherwise noted. |
| Concentrations | 10 μmol/L |
| Incubation time | 24 or 48 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/cAJcl-nu/nu mice |
| Formulation | DMSO |
| Dosages | 3.6 mL/kg/day |
| Administration | i.v. |
| Molecular Weight | 368.31 |
| Formula | C20H13FO6 |
| CAS Number | 1223397-11-2 |
| Solubility (25°C) | 63 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GLUT Products |
|---|
| STF-31
STF-31 is a selective glucose transporter GLUT1 inhibitor, with an IC50 of 1 μM. STF-31 is also a NAMPT inhibitor. |
| 1,9-Dideoxyforskolin
1,9-Dideoxyforskolin is a inactive analog of forskolin |
| Dihydrokainic acid
Dihydrokainic acid is a selective inhibitor of the GLT-1 glutamate transporter. |
| BAY-876
BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1 with an IC50 of 2 nM. BAY-876 is also a potent blocker of glycolytic metabolism and ovarian cancer growth. BAY-876 can induce the formation of disulfide bonds in actin cytoskeletal proteins, leading to the occurrence of cellular disulfidptosis. |
| BAY-588
BAY-588 is an inactive control probe for BAY-876. |
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