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Glutaminase-IN-1 is an inhibitor of glutaminase 1 (GLS1), also known as kidney-type (K-type) glutaminase (IC50 = 1 nM) and a selenium-containing derivative of CB-839 (Item No. 22038).1 It is selective for GLS1 over glutamate dehydrogenase (GDH; IC50 = >13 µM). It inhibits the proliferation of A549 lung, H22 liver, Caki-1 kidney, and HCT116 colon cancer cells (IC50s = 0.017, 6.78, 0.019, and 0.009 µM, respectively). Glutaminase-IN-1 (10 µM) induces the production of reactive oxygen species (ROS) in A549 cells. It decreases tumor weight in an HCT116 mouse xenograft model when administered at a dose of 10 mg/kg.
WARNING This product is not for human or veterinary use.
1. Novel 1,3,4-