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GSK656 is a potent Mtb LeuRS inhibitor, shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). GSK656 is highly selective for the Mtb LeuRS enzyme with IC50 of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. In addition, GSK656 exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads.
| Molecular Weight | 293.94 |
| Formula | C10H13BClNO4.HCl |
| CAS Number | 2131798-13-3 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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