GSK-LSD1

GSK-LSD1 is a potent, selective, and irreversible small molecule inhibitor of lysine specific demethylase 1 (LSD1; also known as KDM1A), a histone demethylase involved in epigenetic regulation. It was developed by GlaxoSmithKline as a chemical probe for research and potential therapeutic applications. GSK-LSD1 inhibits LSD1 with an IC50 of 16 nM and demonstrates over 1000-fold selectivity against related FAD-dependent enzymes such as LSD2, MAO-A, and MAO-B. The compound induces gene expression changes in cancer cell lines (average EC50 <5 nM) and inhibits their proliferation. It has been studied primarily in the context of cancer biology—especially acute myeloid leukemia (AML)—and has also shown effects on food intake, body weight reduction, insulin sensitivity improvement, and glycemic control in preclinical models[2][3][4][5].

Brand names

GSK-LSD1GSK-LSD-1GSK-LSD 1

Other names

N-[(1R,2S)-2-phenylcyclopropyl]piperidin-4-amineGSK LSD1 dihydrochloride1431368-48-7