Catalog No.: PC-26613Not For Human Use, Lab Use Only.
ERG240 (ERG-240) is a potent, selective, orally active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor, inhibits recombinant BCAT1 with an IC50 of 0.1-1 nM, with no inhibition on BCAT2.
ERG240 (ERG-240) is a potent, selective, orally active branched-chain amino acid aminotransferase 1 (BCAT1) inhibitor, inhibits recombinant BCAT1 with an IC50 of 0.1-1 nM, with no inhibition on BCAT2. ERG240 (3 h, 20 mM) treatment induced reduction in IRG1 mRNA levels but not HIF1A and IL1B in LPS-stimulated cells, resulted in decreased itaconate levels. ERG240 showed comparable inhibitory effect on IRG1 expression in TNF-stimulated human macrophages and long-term exposure (24 h) to LPS and ERG240 resulted in reduced IL-1β levels. ERG240 significantly reduced TNF and NOS2 but not IL6 and PTGS2 expression levels in human macrophages. ERG240 blocked itaconate production in vivo and polarizes peritoneal macrophages. ERG240 reduced the severity of crescentic glomerulonephritis in rats and CIA in mice.
Physicochemical Properties
M.Wt
166.15
Formula
C7H11NaO3
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
Sodium 4-methyl-5-oxohexanoate
References
1. Papathanassiu AE, et al. Nat Commun. 2017 Jul 12;8:16040.
