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GSK656 is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.

GSK656 is highly selective inhibitor for Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM, and shows IC50s of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. GSK656 exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. GSK656 also exhibits EC50s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis[1].

GSK656 shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED99 of 0.4 mg/kg[1].

[1]. Li X, et al. Discovery of a Potent and Specific M. tuberculosis Leucyl-tRNA Synthetase Inhibitor: (S)-3-(Aminomethyl)-4-chloro-7-(2-hydroxyethoxy)benzo[c][1,2]oxaborol-1(3H)-ol (GSK656). J Med Chem. 2017 Oct 12;60(19):8011-8026.

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