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Glutaminase C inhibitor 11 is an inhibitor of glutaminase C (GAC).1 It inhibits GAC enzyme activity (EC50 = 10.64 nM) and reduces the viability of A549 non-small cell lung cancer (NSCLC) cells (IC50 = 4.025 nM). Glutaminase C inhibitor 11 (0.1 and 1 µM) reduces colony formation by, and intracellular glutamate levels in, A549 cells. In vivo, glutaminase C inhibitor 11 (100 mg/kg) reduces tumor growth in an A549 mouse xenograft model.
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1. Targeting the subpocket enables the discovery of thiadiazole-