Glutamate Dehydrogenase 1 inhibitor / 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 lead 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 us a useful tool for proof of principal studies.
Biochemicals & reagents
64302-87-0
Purpurin analog
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
-20°C
TARGET: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH) -- PATHWAY: Redox; Anoikis; Amino acid metabolism; Proliferation -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer