Epetraborole (hydrochloride)

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[1][2][3].

Product Specifications

CAS Number

[1234563-16-6]

Product Name Alternative

GSK2251052 hydrochloride

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Aminoacyl-tRNA Synthetase; Bacterial

Type

Reference compound

Related Pathways

Anti-infection; Metabolic Enzyme/Protease

Applications

COVID-19-immunoregulation

Field of Research

Infection

Assay Protocol

https://www.medchemexpress.com/Epetraborole-hydrochloride.html

Purity

99.62

Solubility

DMSO : 200 mg/mL (ultrasonic) |H2O : ≥ 28 mg/mL

Smiles

OCCCOC1=C(B(O)O[C@@H]2CN)C2=CC=C1.[H]Cl

Molecular Formula

C11H17BClNO4

Molecular Weight

273.52

Precautions

H302, H315, H319, H335

References & Citations

[1]Goldstein EJ, et al. Comparative in vitro activities of GSK2251052, a novel boron-containing leucyl-tRNA synthetase inhibitor, against 916 anaerobic organisms. Antimicrob Agents Chemother. 2013 May;57 (5) :2401-4.|[2]O'Dwyer K, et al. Bacterial resistance to leucyl-tRNA synthetase inhibitor GSK2251052 develops during treatment of complicated urinary tract infections. Antimicrob Agents Chemother. 2015 Jan;59 (1) :289-98.|[3]Sutcliffe JA. Antibiotics in development targeting protein synthesis. Ann N Y Acad Sci. 2011 Dec;1241:122-52.