GSK2879552 is a first-in-class, orally bioavailable, potent, selective, and mechanism-based irreversible inhibitor of Lysine specific demethylase 1 (LSD1). LSDI, a histone H3K4me1/2 demethylase found in various transcriptional co-repressor complexes, including Histone Deacetylases (HDAC1/2) and Co-Repressor for Element-1-Silencing Transcription factor (CoREST). Studies have implicated that LSD1 is a key regulator of the epigenome that modulates gene expression through post-translational modification of histones and through its presence in transcriptional complexes, and is overexpressed in certain tumor cells. Inhibition of LSD1 enhances H3K4 methylation and increases the expression of tumor-suppressor genes.

KEYWORDS: GSK2879552 dihydrochloride | Supplier | LSD1 inhibitor | GSK-2879552 | GSK 2879552 | CT-GSK287 | CAS [1902123-72-1] | [1401966-69-5] | Histone | Histone demethylase | Inhibitor | Enzymes