Namoline is a γ-pyrone compound that functions as a selective and reversible inhibitor of Lysine-specific demethylase 1 (LSD1) with an IC50 of 51 μM in an HRP-coupled enzymatic assay. By impairing LSD1 demethylase activity, Namoline effectively inhibits cell proliferation. Due to its characteristics, Namoline holds promise for research pertaining to androgen-dependent prostate cancer.

Namoline (50 μM) suppresses androgen-stimulated growth of LNCaP cells after 24, 48, and 72 hours of treatment, as shown in source [1]. It also selectively disrupts the demethylation of H3K9me1 and H3K9me2, which is induced by the AR agonist R1881 (1 nM) in LNCaP cells, according to the same source [1]. Under these conditions, Namoline (50 μM) does not influence the enzymatic activities of monoamine oxidases (MAOs) [1].

Namoline (0.02 mg; ip; daily) significantly inhibits the growth of xenograft tumors in nude mice implanted with LNCaP cells[1].