aminoacyl-trna synthetase

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.

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

Aminoacyl tRNA synthetase-IN-3 (compound 36K3) is an inhibitor of lysyl-tRNA synthetase (PfLysRS) in Plasmodium falciparum with an IC50 value of 59.2 nM. It works by occupying the ATP and L-lysine binding sites of PfLysRS, thereby inhibiting its activity. This compound is a potential candidate for antimalarial drug development.

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].

Gln-AMS(TFA) inhibits glutaminyl-tRNA synthetase (GlnRS) with a Ki of 1.32 μM. Gln-AMS (TFA) is a type Ia aminoacyl-tRNA synthetase (AARS) inhibitor.

Antibacterial agent 91, a triple-site aminoacyl-tRNA synthetase (aaRS) inhibitor, demonstrates efficacy with an IC50 of 2.10 μM against Salmonella enterica threonyl-tRNA synthetase (Se ThrRS), thereby exhibiting antibacterial activities.

Antibacterial agent 92, a triple-site aminoacyl-tRNA synthetase (aaRS) inhibitor, demonstrates a potent antibacterial effect by inhibiting Salmonella enterica threonyl-tRNA synthetase (SeThrRS) with an IC50 of 0.58 μM.