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

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

LeuRS-IN-1 hydrochloride 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 hydrochloride 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 hydrochloride in HepG2 cells was 65.8 μM (48 h). [2]

In animal experiments, LeuRS-IN-1 hydrochloride 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]