An LSD1 inhibitor
Lysine-specific demethylase inhibitor (1C) (LSD inhibitor (1C)) is an inhibitor of LSD1, a repressive demethylase selective for histone H3 lysine 4 (H3K4).1,2 LSD inhibitor (1C) inhibits LSD1 activity by 85.9% when used at a concentration of 10 µM.1 It increases the level of H3K4 methylation, including H3K4me1 and H3K4me2 but not H3K9me2 levels, in HCT116 human colon carcinoma cells.2 LSD 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)
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