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LCS3 is an inhibitor of glutathione reductase (GR) and thioredoxin reductase (TrxR; IC50s = 3.3 and 3.8 µM, respectively).1 It decreases the glutathione (GSH) to oxidized GSH (GSSG) ratio in NCI H1650 and H23 lung adenocarcinoma cells in a concentration-dependent manner. LCS3 (3 µM) induces apoptosis in NCI H1650 and H23 cells but not non-transformed HPL1D lung epithelial cells. It is also active against M. tuberculosis (MIC = 0.098 µM).2
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1. Characterization of a small molecule inhibitor of disulfide reductases that induces oxidative stress and lethality in lung cancer cells. Cell Rep. 38(6), 110343 (2022).
2. Optimization of N-