GSK656 HCl (GSK3036656, GSK070)

Description: GSK656 (GSK-3036656 and GSK-070) is a novel and potent antitubercular agent which acts as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 uM. There is an urgent need to develop new and safer antitubercular agents that possess a novel mode of action. GSK3036656 (abbreviated as GSK656) shows potent inhibition of Mtb LeuRS (IC50 = 0.20 uM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 uM). Additionally, it is highly selective for the Mtb LeuRS enzyme with IC50 of > 300 uM and 132 uM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. In addition, it exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads. This compound has been progressed to clinical development for the treatment of tuberculosis.

References: J Med Chem. 2017 Oct 12; 60(19):8011-8026.

Related CAS #: 2131798-12-2 (free base); 2131798-13-3 (HCl)