Hu, Youtian Wang, Lu Han, Xu Zhou, Yueyang Zhang, Tonghui Wang, Li Hong, Ting Zhang, Wei Guo, Xun-Xiang Sun, Jielin Qi, Yingxin Yu, Jing Liu, Hong Wu, Fang Discovery of a Bioactive Inhibitor with a New Scaffold for Cystathionine γ‑Lyase We identify three submicromolar inhibitors with new chemical scaffolds for cystathionine γ-lyase (CSE) by a tandem-well-based high-throughput assay. NSC4056, the most potent inhibitor with an IC<sub>50</sub> of 0.6 μM, which is also known as aurintricarboxylic acid, selectively binds to Arg and Tyr residues of CSE active site and preferably inhibits the CSE activity in cells rather than cystathionine β-synthase (CBS), the other H<sub>2</sub>S-generating enzyme. Moreover, NSC4056 effectively rescues hypotension in hemorrhagic shock rats. 0.6 μ M;IC 50;NSC 4056;cystathionine β- synthase;tandem-well-based high-throughput assay;chemical scaffolds;Tyr residues;hemorrhagic shock rats;submicromolar inhibitors;rescues hypotension;CSE activity;cystathionine γ- lyase;Bioactive Inhibitor;aurintricarboxylic acid;H 2 S-generating enzyme;New Scaffold;CBS 2018-12-18
    https://acs.figshare.com/articles/dataset/Discovery_of_a_Bioactive_Inhibitor_with_a_New_Scaffold_for_Cystathionine_Lyase/7533248
10.1021/acs.jmedchem.8b01720.s003