Namoline

Names

[ Name ]:
Namoline

Biological Activity

[Description]:

Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Demethylase

[In Vitro]

Namoline (50 μM; 24, 48, 72 hours) reduces androgen-induced proliferation of LNCaP cells[1]. Namoline (50 μM) specifically impairs AR agonist R1881-induced (1 nM) demethylation of H3K9me1 and H3K9me2 in LNCaP cells[1]. Namoline (50 μM) does not affect the enzymatic activities of MAOs under these conditions[1].

[In Vivo]

Namoline (0.02 mg;ip; daily) severely blunts xenograft tumor growth in nude mice with LNCaP cells[1].

[References]

[1]. Dominica Willmann, et al. Impairment of prostate cancer cell growth by a selective and reversible lysine-specific demethylase 1 inhibitor. Int J Cancer. 2012 Dec 1;131(11):2704-9.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₀H₃ClF₃NO₄

[ Molecular Weight ]:
293.58

Related Compounds

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