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.
R162 is a glutamate dehydrogenase 1 inhibitor for the treatment of cancer. A useful bioactive chemical compound.
ChEBI: 2-allyl-1-hydroxy-9,10-anthraquinone is a monohydroxyanthraquinone that is 9,10-anthraquinone in which the hydrogens at positions 1 and 2 are replaced by a hydroxy and an allyl group, respectively. It has a role as an EC 1.4.1.3 {glutamate dehydrogenase [NAD(P)(+)]} inhibitor.
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
