CAS 1448428-04-3: Selonsertib

Selonsertib (GS-4997), an oral ASK1 inhibitor, may have anti-inflammatory, anti-fibrotic, and anti-cancer effects.

Selonsertib is a highly selective inhibitor of the ATP-binding cassette transporter (ABCA1) that belongs to the class of glp-1 analogues. It is used in combination with other drugs for the treatment of bowel disease, autoimmune diseases, and skin cancer. Selonsertib has been shown to be active against a number of cell types and is also effective in models of metabolic disorders such as hepatic steatosis and kidney fibrosis. Selonsertib blocks ABCA1 by binding to its ATP-binding site, inhibiting cholesterol efflux from cells. This drug may work by restoring mitochondrial membrane potential, which may help prevent or reverse cellular damage caused by oxidative stress.

Selonsertib

Applications Selonsertib is an apoptosis signal-regulating kinase 1 (ASK1) inhibitor with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. Selonsertib interacts with the catalytic kinase domain of ASK1 and prevents its phosphorylation and activation. As a result, the expression of genes involved in fibrosis, cellular proliferation, and apoptosis are down regulated. References Nelson, C. H. et al.: Clin Pharmacol Ther. 98, 630 (2015); Lin, J. H., et al.: Nephron. 129, 29 (2015)

5-(4-Cyclopropyl-1H-Imidazol-1-Yl)-2-Fluoro-N-(6-(4-Isopropyl-4H-1,2,4-Triazol-3-Yl)Pyridin-2-Yl)-4-Methylbenzamide