Epetraborole
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[1][2][3].
Product Specifications
CAS Number
1093643-37-8
Product Name Alternative
GSK-2251052; AN 3365
UNSPSC
12352005
Hazard Statement
H315-H319-H320
Target
Aminoacyl-tRNA Synthetase; Bacterial
Type
Reference compound
Related Pathways
Anti-infection; Metabolic Enzyme/Protease
Field of Research
Infection
Assay Protocol
https://www.medchemexpress.com/epetraborole.html
Solubility
10 mM in DMSO
Smiles
OCCCOC1=C2C([C@H](OB2O)CN)=CC=C1
Molecular Formula
C11H16BNO4
Molecular Weight
237.06
Precautions
P264-P280-P302+P352-P305+P351+P338-P362
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 3
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