R162

R162 is a potent and selective small molecule inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), an enzyme involved in cellular metabolism. By inhibiting GDH1 activity (Ki ≈ 28.6 µM), R162 disrupts metabolic processes critical for cancer cell proliferation and survival. It has demonstrated anti-cancer properties in vitro by reducing intracellular fumarate levels, attenuating glutathione peroxidase activity, increasing reactive oxygen species (ROS) production, and inducing apoptosis—particularly in LKB1-deficient non-small cell lung cancer cells. In vivo studies show that R162 significantly inhibits tumor growth and metastasis in xenograft mouse models without causing significant toxicity to normal tissues[4][5][6][8]. The compound is primarily used as a research tool to study cancer metabolism.

Other names

2-Allyl-1-hydroxy-9,10-anthraquinoneGDH1 InhibitorGDH-1 InhibitorGDH 1 InhibitorGlutamate Dehydrogenase 1 InhibitorGLUD1 InhibitorGLUD-1 InhibitorGLUD 1 Inhibitor