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BAY-876 is a potent, highly selective, cell-permeable inhibitor of glucose transporter GLUT1. It had an IC50 value of 2 nM in vitro and inhibited glucose uptake by Hela-MaTu cells with an IC50 value of 3.2 nM. BAY-876 was at least 130-fold selective for GLUT1 relative to GLUT2, GLUT3, GLUT4 and a panel of 18 kinases and 68 proteins. 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.
| Cell Experiment | |
|---|---|
| Cell lines | B16F10 cells |
| Preparation method | To test if BAY-876 induces apoptosis, HNSCC cells were treated with BAY-876 over 15 h with fluorescent CellEvent dye to measure caspase-3 and/or -7 cleavage. |
| Concentrations | 1, 50, 100 μM |
| Incubation time | 15 h |
| Animal Experiment | |
|---|---|
| Animal models | Nude mice |
| Formulation | Physiological saline solution containing a 6.25% (V/V) concentration of Tween 80 |
| Dosages | 5 mg/kg |
| Administration | Oral administration |
| Molecular Weight | 496.42 |
| Formula | C24H16F4N6O2 |
| CAS Number | 1799753-84-6 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Qin Wu, et al. GLUT1 inhibition blocks growth of RB1-positive triple negative breast cancer
| 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. |
| WZB117
WZB117 is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 μM. |
| 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-588
BAY-588 is an inactive control probe for BAY-876. |
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