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Lysine-specific Demethylase Inhibitor (1C) (Synonyms: KDM1 Inhibitor I|LSD1 Inhibitor)

Catalog No.GC13534

lysine-specific demethylase Inhibitor

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Lysine-specific Demethylase Inhibitor (1C) Chemical Structure

Cas No.: 927019-63-4

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10mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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
Synonyms KDM1 Inhibitor I|LSD1 Inhibitor
Chemical Name N,N'-dimethyl-15-(methylimino)-2,6,10,14,16-pentaazaheptadecanimidamide
Canonical SMILES CN/C(NCCCNCCCNCCCN/C(NC)=N/C)=N\C
Formula C15H36N8 M.Wt 328.5
Solubility Soluble in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 36 reference(s) in Google Scholar.)

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