Aminoacyl-tRNA Synthetase Inhibitor

Mupirocin is an antibiotic. Mupirocin inhibits bacterial isoleucyl-tRNA synthetase, blocking protein synthesis. Mupirocin has high activity against Gram-positive bacteria such as Staphylococcus and Streptococcus, as well as some Gram-negative bacteria (such as Haemophilus influenzae). Mupirocin can be used in the research of diseases such as skin infections (such as MRSA infections) and chronic sinusitis.

L-Histidinol dihydrochloride is an orally active histidyl-tRNA synthetase inhibitor. L-Histidinol dihydrochloride interferes with the initiation stage of protein synthesis, thus affecting cell proliferation and metabolism. L-Histidinol dihydrochloride has the effect of modulating the sensitivity of tumor cells to chemotherapeutic agents. L-Histidinol dihydrochloride reduces the toxicity of certain chemotherapeutic agents to normal tissues and enhance the sensitivity of tumor cells to chemotherapeutic agents.

Gln-AMS is an aminoacyl-tRNA synthetases (AARS) inhibitor, which binds the A-domain within the NRPS enzymes.

Epetraborole (GSK2251052) hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor (IC₅₀=0.31 μM), thereby inhibiting protein synthesis. Epetraborole hydrochloride can be used in multidrug-resistant gram-negative pathogens infection research.

BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC₅₀=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (K_d=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated?MTOR?mutants and the growth of rapamycin-resistant cancer cells.?BC-LI-0186 is a promising agent for lung cancer research.

BC-DXI-495 is a AIMP2-DX2 inhibitor. BC-DXI-495 disrupts the interaction of HSP70 and destabilizes DX2. BC-DXI-495 induces DX2 degradation via Siah1-mediated ubiquitination. BC-DXI-495 exerts tumor suppressive activity in cancer cells. BC-DXI-495 serves as a chemical probe to elucidate the mechanism of action of arylsulfonamide-based DX2 inhibitors. BC-DXI-495 can be used in lung cancer research.

Mupirocin lithium is an antibiotic. Mupirocin lithium inhibits bacterial isoleucyl-tRNA synthetase, blocking protein synthesis. Mupirocin lithium has high activity against Gram-positive bacteria such as Staphylococcus and Streptococcus, as well as some Gram-negative bacteria (such as Haemophilus influenzae). Mupirocin lithium can be used in the research of diseases such as skin infections (such as MRSA infections) and chronic sinusitis.

GlyRS-IN-1 is a glycyl-tRNA synthase (GlyRS) inhibitor extracted from patent WO 2017066459 A1. GlyRS-IN-1 can also inhibit the growth of bacteria.

Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC₅₀ of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.

Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.

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

Arg-AMS (compound 24) is a potent nanomolar inhibitor of arginyl tRNA synthetase, which displays tightly bound inhibitory characteristics for the A-domains in non-ribosomal peptide synthetases (NRPS) enzymes.

Aminoacyl tRNA synthetase-IN-1 (IleSA) is an inhibitor of bacterial aminoacyl-tRNA synthetase (aaRS). Aminoacyl tRNA synthetase-IN-1 is applicable to studies on bacterial infections.

LysRs-IN-2 is a lysyl-tRNA synthetase (KRS) inhibitor with IC₅₀s of 0.015 μM and 0.13 μM for Plasmodium falciparum lysyl-tRNA synthetase (PfKRS) and Cryptosporidium parvum lysyl-tRNA synthetase (CpKRS), respectively.

Bersiporocin (DWN12088) is an orally effective prolyl-tRNA synthetase (PRS) inhibitor. Bersiporocin exerts antifibrotic effects by inhibiting collagen synthesis. Bersiporocin can be used in the research of pulmonary fibrosis.

NP-BTA is an allosteric inhibitor for glutaminyl-tRNA synthetase (GlnRS). NP-BTA exhibits antifungal efficacy against Candida albicans, with MIC₅₀ of 6.25 μM.

LysRs-IN-1 is a Lysyl-tRNA synthetase (LysRs) inhibitor.

Glu-AMS TEA is a competitive inhibitor of Escherichia coli glutamyl-tRNA synthetase (GluRS), with the K_i of 2.8 nM.

BC-DXI-843 is a potent and specific AIMP2-DX2 inhibitor with an IC₅₀ of 0.92 μM, more than 100-fold selectivity over AIMP2 (IC₅₀ >100 μM) in a luciferase assay. BC-DXI-843 acts as a promising lead targeting AIMP2-DX2 in lung cancer.

Epetraborole (GSK2251052) is a leucyl-tRNA synthetase (LeuRS) inhibitor (IC₅₀=0.31 μM), thereby inhibiting protein synthesis. Epetraborole can be used in multidrug-resistant gram-negative pathogens infection research.