S2172

S2172 is a novel, brain-penetrant small molecule inhibitor of Lysine-specific demethylase 1 (LSD1), an epigenetic enzyme that regulates gene expression by demethylating histone H3 lysine 4 (H3K4) and lysine 9 (H3K9). Developed by researchers at Nagoya University, S2172 is being investigated for the treatment of glioblastoma multiforme (GBM). It demonstrates potent growth inhibition in glioblastoma stem cells (GSCs) and differentiated GBM cells in vitro, outperforming other LSD1 inhibitors like iadademstat (Ory-1001) and seclidemstat (CC-90011) in certain cell lines. Its mechanism involves the suppression of the Myc oncogene through the alteration of H3K4 methylation patterns. While showing strong in vitro activity, its in vivo efficacy appears more restricted to stem-like tumor-propagating cells.