| Description | Ganfeborole HCl (GSK3036656 HCl) is a small molecule compound with anti-tuberculosis activity and is an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS; IC50: 0.2 μM). |
| In vitro | GSK3036656 显示出对 Mtb LeuRS 的强效抑制作用（IC50=0.20 μM）和体外抗结核活性（Mtb H37Rv MIC = 0.08 μM）。此外，它对 Mtb LeuRS 酶高度选择性，分别对人类线粒体 LeuRS 和人类胞质 LeuRS 的 IC50 分别为>300 μM 和132 μM[1]。 |
| In vivo | GSK3036656 (0.4 mg/kg) 在小鼠 TB 感染模型中表现出显著的药代动力学特性和对 Mtb 的疗效[1]。 |
| Target activity | LeuRS (Mtb):0.2 μM |
| Synonyms | GSK3036656 HCl, GSK656 HCl |
| molecular weight | 293.94 |
| Molecular formula | C10H14BCl2NO4 |
| CAS | 2131798-13-3 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (170.07 mM), Sonication is recommended. |
| References | 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. |