LeuRS-IN-1 is an orally active and potent Mycobacterium tuberculosis leucyl-tRNA synthetase inhibitor with anti-leukemic and anti-malarial activity, inhibits M.tb LeuRS, inhibits HepG2 protein synthesis, and can be used in leukemia research.

LeuRS (Mtb):0.075 μM (Kd), HepG2 protein synthesis:19.6 μM (EC50), HepG2 cells:65.8 μM (toxicity EC50), LeuRS (Mtb):0.06 μM, HepG2 protein synthesis:38.8 μM

LeuRS-IN-1 showed high inhibitory activity against leucyl tRNA synthetase of Mycobacterium tuberculosis (M.tb) with IC50 and Kd values of 0.06 μM and 0.075 μM, respectively, and a MIC of 0.02 μg/mL against M.tb H37Rv strain. [1]
LeuRS-IN-1 was less effective in inhibiting human cytoplasmic LeuRS and HepG2 protein synthesis, with IC50 and EC50 values of 38.8 μM and 19.6 μM, respectively, and the toxicity EC50 of LeuRS-IN-1 in HepG2 cells was 65.8 μM (48 h). [2]

In animal experiments, LeuRS-IN-1 administered orally at 100 mg/kg per day for 14 consecutive days reduced the lung colony units of acute tuberculosis mice, while 33 mg/kg administered orally 5 days per week for 4 consecutive weeks reduced the lung and spleen colony units of chronic tuberculosis mice. [1]