LSD1-IN-32 (compound 11e) is a potent inhibitor of LSD1, with an IC50 value of 0.99 µM. It effectively impedes RANKL-induced osteoclastogenesis, bone resorption, and F-actin ring formation, indicating its potential use in osteoporosis research.

LSD1-IN-32 (compound 11e) influences osteoclastogenesis by increasing methylation levels in a dose-dependent manner at concentrations of 1.25, 2.5, and 5 µM. It inhibits RANKL-induced osteoclastogenesis, bone resorption, and F-actin ring formation at 0.25, 0.5, 1, 2, and 4 µM. Additionally, at 2 µM over 0, 1, 2, and 4 days, it decreases mRNA expression levels of RANKL-induced genes including Acp5, Nfatc1, Oscar, Dc-stamp, Atp6v0d2, and Ctsk. Furthermore, LSD1-IN-32 at 0.5, 1, 2, and 4 µM suppresses the expression of p-LSD1, p-IκB, and p-NFκB in the osteoclastogenesis process induced by RANKL.

LSD1-IN-32 (5, 10 mg/kg) inhibited osteoclast-driven bone loss induced by OVX in mice.