Lysine-specific Demethylase Inhibitor (1C)

Lysine-specific Demethylase Inhibitor (1C)

Catalog Number:
L002372862APE
Mfr. No.:
APE-C3630
Price:
$297
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      • Overview
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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.

      • Properties
        • Alternative Name
          KDM1 Inhibitor I|LSD1 Inhibitor; N,N'-dimethyl-15-(methylimino)-2,6,10,14,16-pentaazaheptadecanimidamide
          CAS Number
          927019-63-4
          Molecular Formula
          C15H36N8
          Molecular Weight
          328.5
          Purity
          98.00%
          Solubility
          Soluble in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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