Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).^1,2LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 µM.¹It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.²LSD inhibitor (1C) also induces re-expression of the Wnt signaling pathway proteins secreted frizzle-related protein 1 (SFRP1), SFRP4, and SFRP5, as well as the transcription factor GATA5, which are aberrantly silenced in HCT116 cells.

1.Sharma, S.K., Wu, Y., Steinbergs, N., et al.(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulatorsJ. Med. Chem.53(14)5197-5212(2010) 2.Huang, Y., Greene, E., Murray Stewart, T., et al.Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genesProc. Natl. Acad. Sci. U.S.A.104(19)8023-8028(2007)