Seclidemstat mesylate (SP-2577) is a highly effective and reversible inhibitor of KDM1A (LSD1), with a Ki of 31 nM and an IC50 of 13 nM. It shows promising potential in enhancing antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer and exhibits inhibitory effects on virus production, viral DNA replication, and late gene expression. Additionally, seclidemstat mesylate is a valuable tool for studying Ewing Sarcoma in research settings.

LSD1:13 nM (IC50), LSD1:31 nM (Ki)

Seclidemstat mesylate, over a period of 72 hours, effectively inhibits the proliferation of various tumor cells with mutations in the SWI/SNF complex, achieving an IC50 range of 0.013 to 2.819 μM across multiple cell lines (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15). Additionally, it enhances the expression and activation of endogenous retroviruses (ERVs) and the IFNβ signaling pathway specifically in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434). At a concentration of 3 μM, Seclidemstat mesylate also upregulates PD-L1 expression in the SCCOHT COV 434 pIND 20 BRG1-2.7 cell line.