Lysine-specific Demethylase Inhibitor (1C) (hydrochloride)

An LSD1 inhibitor

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库存: 现货

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1mg

￥737.00

590.00

- +
5mg

￥2037.00

1630.00

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10mg

￥3350.00

2680.00

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Background

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)