Lysine-specific Demethylase Inhibitor (1C)
目录号 : KG10463
CAS No. : 927019-63-4
纯度 : 98%
Lysine-specific Demethylase Inhibitor (1C) is a lysine-specific demethylase inhibitor.
Lysine-specific demethylase 1 (LSD1) is the first of several protein lysine demethylases identified. Through a FAD-dependent oxidative reaction, LSD1 could specifically remove histone H3K4me2 to H3K4me1 or H3K4me0. When forming a complex with androgen receptor, LSD1 alters its substrates to H3K9me2. The LSD1 complex regulates a coordinated histone modification switch via enzymatic activities and histone modification readers.
In vitro: Lysine-specific Demethylase Inhibitor (1C) was identified as a bisguanidine polyamine analogue exhibiting noncompetitive and specific LSD1 inhibition, with 14.1% in vitro LSD1 activity at 10 μM. Lysine-specific Demethylase Inhibitor (1C) at 0.25 μM to 10 μM could significantly and dose-dependently increase methylation at the histone 3 lysine 4 chromatin mark, H3K4me1 and H3K4me2, without affecting global H3K9me2 levels in HCT116 human colon carcinoma cells. Lysine-specific Demethylase Inhibitor (1C) could also induce expression of several epigenetically silenced genes, such as SFRP1, SFRP4, SFRP5, and GATA5, particularly in the case of SFRP4 and SFRP5 .
In vivo: Currently, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted
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分子式 |
C15H36N8
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分子量 |
328.5
|
CAS号 |
927019-63-4
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中文名称 |
N,N'-dimethyl-15-(methylimino)-2,6,10,14,16-pentaazaheptadecanimidamide
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储存方式 |
Store at -20°C
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