SB-204990

SB-204990 is a small molecule research compound that functions as a γ-lactone prodrug of SB-201076, a potent and specific inhibitor of ATP citrate lyase (ACLY). Developed by SmithKline Beecham (now GSK), it is orally active and cell-permeable, with a Ki of approximately 1 μM against human and rat ACLY. By inhibiting ACLY, the enzyme responsible for converting mitochondrial-derived citrate into oxaloacetate and acetyl-CoA, SB-204990 suppresses the synthesis of cholesterol and fatty acids. It has been investigated for therapeutic applications in metabolic diseases, such as hyperlipidemia and hypercholesterolemia, and more recently in oncology, where it has shown potential in suppressing the growth of cancer cells (e.g., small cell lung cancer liver metastasis) by disrupting metabolic-epigenetic reprogramming and stem-like states.

Other names

SB 204990SB204990SB-204990