R162 is a cell-permeable, nontoxic selective inhibitor of Glutamate Dehydrogenase 1 (GDH1), (Ki = 28.6 µM) which is an upregulated enzyme in human cancers. It shows selectivity over other NADPH-dependent enzymes such as 6-phosphogluconate dehydrogenase (6PGD) and Fumarate hydratase (FH). It shows reduced levels of intracellular fumarate levels and Glutathione peroxidase (GPx) activity with an increase in mitochondrial ROS levels. Decreases the tumor growth and inhibits the cancer cell proliferation of H1299 and primary leukemia cells.