R162

R162 is an inhibitor of glutamate dehydrogenase 1 (GDH1, IC50 = 23 µM). It decreases intracellular fumarate levels and increases the production of mitochondrial reactive oxygen species (ROS) in human H1299 lung and MDA-MB-231 breast cancer cells. R162 (10-40 µM) inhibits proliferation in a panel of human cancer cell lines, including lung, breast, and leukemia cells, but not normal human HaCaT keratinocytes, MRC-5 lung fibroblasts, or foreskin fibroblasts. It reduces tumor growth and intratumoral GDH1 activity in an H1299 mouse xenograft model when administered at a dose of 20 mg/kg. R162 also reduces liver metastasis in a liver kinase B1-deficient lung cancer patient-derived xenograft (PDX) mouse model when administered at the same dose.Formal Name: 1-hydroxy-2-(2-propen-1-yl)-9,10-anthracenedione. CAS Number: 64302-87-0. Molecular Formula: C17H12O3. Formula Weight: 264.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1 mg/ml, DMSO: slightly soluble, Ethanol: slightly soluble. lambdamax: 223, 253 nm. SMILES: O=C1C2=C(C=CC(CC=C)=C2O)C(C3=CC=CC=C31)=O. InChi Code: InChI=1S/C17H12O3/c1-2-5-10-8-9-13-14(15(10)18)17(20)12-7-4-3-6-11(12)16(13)19/h2-4,6-9,18H,1,5H2. InChi Key: IMUBGIOLZQTIGI-UHFFFAOYSA-N.