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ERG240 is a selective inhibitor of branched-chain aminotransferase 1 (BCAT1) with an IC50 of 0.1-1nM. ERG240 leads to decreased oxygen consumption and glycolysis through the down regulation of IRG1 expression, which leads to decrease itaconate production in human macrophages. EGR240 can be used for the research of cancer, rheumatoid arthritis, and bone disease.
ERG240 suppresses production of IRG1 and itaconate in mice and contributes to a less proinflammatory transcriptome signature. Oral administration of ERG240 reduces the severity of collagen-induced arthritis in mice and crescentic glomerulonephritis in rats, in part by decreasing macrophage infiltration.
| Molecular Weight | 166.15 |
| Formula | C7H11NaO3 |
| CAS Number | 1415683-79-2 |
| Solubility (25°C) | DMSO 80 mg/mL Water 80 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
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