R162 | Glutamate dehydrogenase 1 inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 10 mg | $60.00 | ||
| 50 mg | $195.00 |
R162 (64302-87-0) is a selective inhibitor of glutamate dehydrogenase 1 (GDH1), a commonly upregulated enzyme in human cancers (Ki = 28.6 µM). It does not inhibit the activity of other NADPH enzymes such as 6-phosphogluconate dehydrogenase and fumarate hydratase. R162 treatment leads to decreased fumarate levels, lower glutathione peroxidase activity, increased ROS levels and reduced cell proliferation in H1299 and MDA-MB231 cells. R162 sensitizes LKB-1 deficient tumor cells to anoikis induction. R162 treatment (at 20 mg/kg/day) significantly attenuates metastatic potential in a xenograft mouse model.2 GDH1 is a promising antimetastasis target and R162 is a useful tool for proof of principal studies.
References/Citations:
1) Jin et al. (2015), Glutamate Dehydrogenase 1 Signals through Antioxidant Glutathione Peroxidase 1 to Regulate Redox Homeostasis and Tumor Growth; Cancer Cell, 27 257
2) Jin et al. (2018) The PLAG1-GDH1 Axis Promotes Anokis Resistance and Tumor Metastasis through CamKK2-AMPK Signaling in LKB1-Deficient Lung Cancer; Mol. Cell, 69 1
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
R162 (64302-87-0) is a selective inhibitor of glutamate dehydrogenase 1 (GDH1), a commonly upregulated enzyme in human cancers (Ki = 28.6 µM). It does not inhibit the activity of other NADPH enzymes such as 6-phosphogluconate dehydrogenase and fumarate hydratase. R162 treatment leads to decreased fumarate levels, lower glutathione peroxidase activity, increased ROS levels and reduced cell proliferation in H1299 and MDA-MB231 cells. R162 sensitizes LKB-1 deficient tumor cells to anoikis induction. R162 treatment (at 20 mg/kg/day) significantly attenuates metastatic potential in a xenograft mouse model.2 GDH1 is a promising antimetastasis target and R162 is a useful tool for proof of principal studies.
References/Citations:
1) Jin et al. (2015), Glutamate Dehydrogenase 1 Signals through Antioxidant Glutathione Peroxidase 1 to Regulate Redox Homeostasis and Tumor Growth; Cancer Cell, 27 257
2) Jin et al. (2018) The PLAG1-GDH1 Axis Promotes Anokis Resistance and Tumor Metastasis through CamKK2-AMPK Signaling in LKB1-Deficient Lung Cancer; Mol. Cell, 69 1
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1-855-FOCUS21
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