GSK656, also known as GSK3036656 and GSK070, is a potent Mtb LeuRS inhibitor. GSK656 shows potent inhibition of Mtb LeuRS (IC50 = 0.20 μM) and in vitro antitubercular activity (Mtb H37Rv MIC = 0.08 μM). Additionally, it 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, it exhibits remarkable PK profiles and efficacy against Mtb in mouse TB infection models with superior tolerability over initial leads. GSK656 has been progressed to clinical development for the treatment of tuberculosis.
MedKoo Cat#: 576011
Name: GSK-656 free base
CAS#: 2131798-12-2 (free base)
Chemical Formula: C10H13BClNO4
Exact Mass: 257.0626
Molecular Weight: 257.48
Elemental Analysis: C, 46.65; H, 5.09; B, 4.20; Cl, 13.77; N, 5.44; O, 24.86
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 257.48 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
