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REP 8839
- Bederocin
- Soluble in DMSO
- MF: C20H21BrFN3OS
- MW: 450.37
Description
REP 8839 is a selective methionyl-tRNA synthetase (MetRS) inhibitor with antibacterial activity against a range of Gram-positive organisms.
Bacterial MetRS is essential for protein synthesis and represents an antibacterial target. REP 8839 is useful for investigating aminoacyl-tRNA synthetase inhibition, Gram-positive antibacterial activity and resistance mechanisms.
Key Features
- Selective inhibitor of bacterial MetRS
- Blocks methionyl-tRNA charging and protein synthesis
- Antibacterial activity against Gram-positive organisms
- Useful tool for antibiotic mechanism studies
Applications
- MetRS enzyme assays
- Antibacterial screening against Gram-positive bacteria
- Protein synthesis inhibition studies
- Antibiotic resistance mechanism research
More Information
| Parent CAS No. | 757942-43-1 |
|---|---|
| Chemical Name | 2-(3-((4-bromo-5-(1-fluorovinyl)-3-methylthiophen-2-yl)methylamino)propylamino)quinolin-4(1H)-one |
| SMILES | C1C=C2NC(NCCCNCC3SC(C(F)=C)=C(Br)C=3C)=CC(=O)C2=CC=1 |
| MFCD | MFCD13152401 |
| InChi | InChI=1S/C20H21BrFN3OS/c1-12-17(27-20(13(2)22)19(12)21)11-23-8-5-9-24-18-10-16(26)14-6-3-4-7-15(14)25-18/h3-4,6-7,10,23H,2,5,8-9,11H2,1H3,(H2,24,25,26) |
| InChiKey | BGJMKHPWCFXMOW-UHFFFAOYSA-N |
| CID | 9868368 |
| Short Description | MetRS inhibitor |
References
- LS Green et al. Inhibition of Methionyl-tRNA Synthetase by REP8839 and Effects of Resistance Mutations on Enzyme Activity. Antimicrob. Agents Chemother. 2009, 86–94.
- IA Critchley et al. Antibacterial Activity of REP8839, a New Antibiotic for Topical Use. Antimicrob. Agents Chemother. 2005, 49(10), 4247–4252.
- UA Ochsner et al. Mode of Action and Biochemical Characterization of REP8839, a Novel Inhibitor of Methionyl-tRNA Synthetase. Antimicrob Agents Chemother. 2005, 49(10), 4253–4262.
- IA Critchley and UA Ochsner. Recent advances in the preclinical evaluation of the topical antibacterial agent REP8839. Curr. Opin. Chem. Biol. 2008, 12(4), 409-417.
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