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Lysine-specific Demethylase Inhibitor (1C) Sale

(Synonyms: KDM1 Inhibitor I|LSD1 Inhibitor) 目录号 : GC13534

lysine-specific demethylase Inhibitor

Lysine-specific Demethylase Inhibitor (1C) Chemical Structure

Cas No.:927019-63-4

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1mg
¥634.00
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5mg
¥1,697.00
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10mg
¥2,791.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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 [1].

In vivo: Currently, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Sharma SK, Wu Y, Steinbergs N, Crowley ML, Hanson AS, Casero RA, Woster PM.  (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.J Med Chem. 2010 Jul 22;53(14):5197-212.

Chemical Properties

Cas No. 927019-63-4 SDF
别名 KDM1 Inhibitor I|LSD1 Inhibitor
化学名 N,N'-dimethyl-15-(methylimino)-2,6,10,14,16-pentaazaheptadecanimidamide
Canonical SMILES CN/C(NCCCNCCCNCCCN/C(NC)=N/C)=N\C
分子式 C15H36N8 分子量 328.5
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 3.0441 mL 15.2207 mL 30.4414 mL
5 mM 0.6088 mL 3.0441 mL 6.0883 mL
10 mM 0.3044 mL 1.5221 mL 3.0441 mL
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