leucyl-trna synthetase

Aminoacyl tRNA synthetase-IN-1 is an inhibitor of bacterial aminoacyl tRNA synthetase (aaRS).

Isoleucyl tRNA synthetase-IN-2 is a selective and potent inhibitor (Ki: 114 nM) that targets isoleucyl tRNA synthetase (IleRS).

Isoleucyl tRNA synthetase-IN-1 is a selective and potent inhibitor (Ki: 88 nM) that targets isoleucyl tRNA synthetase (IleRS).

Aminoacyl tRNA Synthetase-IN-2 (Compound 14) serves as an inhibitor of aminoacyl-tRNA synthetase (aaRS), presenting potential for the formulation of a novel class of antibiotics [1].

LeuRS-IN-1 hydrochloride is a potent and orally active inhibitor of M. tuberculosis leucyl-tRNA synthetase (M.tb LeuRS). It has IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively, for M.tb LeuRS. Additionally, LeuRS-IN-1 hydrochloride inhibits human cytoplasmic LeuRS with an IC 50 of 38.8 μM and HepG2 protein synthesis with an EC 50 of 19.6 μM.

DS86760016 is a highly effective inhibitor of leucyl-tRNA synthetase (LeuRS), demonstrating potent activity against multidrug-resistant (MDR) Gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Notably, DS86760016 effectively inhibits LeuRS enzymes derived from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, exhibiting IC50 values of 0.38 μM, 0.62 μM, and 0.16 μM, respectively.

Epetraborole is a potent and selective leucyl-tRNA synthetase inhibitor. Epetraborole was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens.

Epetraborole hydrochloride (GSK2251052 hydrochloride) is a potent and selective leucyl-tRNA synthetase inhibitor.

GSK656 (GSK3036656) shows potent inhibition of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS) (IC50 = 0.20 μM) which has potential for the treatment of tuberculosis [1].

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).

LeuRS-IN-1 is a highly potent and orally active inhibitor of the leucyl-tRNA synthetase enzyme derived from Mycobacterium tuberculosis (M.tb LeuRS). It exhibits significant inhibitory activity against M.tb LeuRS with IC 50 and Kd values of 0.06 μM and 0.075 μM, respectively. Additionally, LeuRS-IN-1 effectively inhibits human cytoplasmic LeuRS with an IC 50 value of 38.8 μM and suppresses protein synthesis in HepG2 cells with an EC 50 value of 19.6 μM.

3,5-O-Dicaffeoylquinic acid (Isochlorogenic Acid A) is an isolated compound from Artemisia argyi; its ester derivatives exert anti-leucyl-tRNA synthetase of Giardia lamblia (GlLeuRS) and potential anti-giardial effects. 3,5-O-Dicaffeoylquinic acid (Isochlorogenic Acid A) as a neuraminidase inhibitory ligand in Flos Lonicerae, it has neuroprotective effects on SH-SY5Y cells and senescence-accelerated-prone mice 8 through the up-regulation of phosphoglycerate kinase-1. 3,5-O-Dicaffeoylquinic acid (Isochlorogenic Acid A) also has antioxidant and anti-complementary activities.

Leu-AMS, a leucine analogue and potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, exhibits cytotoxic effects in both cancer and normal cells and hampers bacterial growth. It specifically inhibits LRS's catalytic activity without impacting the leucine-induced activation of mTORC1.

Leu-AMS R enantiomer is the R enatiomer of Leu-AMS. Leu-AMS is a potent leucyl-tRNA synthetase (LRS) inhibitor that inhibits the bacteria growth.

BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM. BC-LI-0186 competitively binds the RagD interaction site of LRS with Kd of 42.1 nM and has no effect on LRS-vps34, LRS-eprs, RagB-RagD association, mTORC1 complex formation. BC-LI-0186 potently inhibits the activity of tumor-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 can be used for lung cancer-related research.

Epetraborole R-Mandelate is a potent and selective leucyl-tRNA synthetase inhibitor.

Isochlorogenic acid A (3,5-Dicaffeoylquinic acid), a natural phenolic acid, exhibits antioxidant and anti-inflammatory properties.