An inhibitor of GLS1 (IC50 = 1 nM), selective for GLS1 over GDH (IC50 = >13 µM), inhibits the proliferation of A549, H22, Caki-1, and HCT116 cancer cells (IC50s = 0.017, 6.78, 0.019, and 0.009 µM, respectively), induces ROS production in A549 cells at 10 µM, decreases tumor weight in an HCT116 mouse xenograft model...

Description: Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine inhibitor of the renal-type glutaminase (KGA) variant, exhibited antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model. Target: transporter. Smiles:...