Seclidemstat mesylate

Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma[1][2].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Demethylase

Ki: 31 nM (LSD1)[1] IC50: 13 nM (LSD1)[1]

Seclidemstat (72 hours) mesylate inhibits SWI/SNF-mutation-dependent tumor cell proliferation with IC50 ranging from 0.013 to 2.819 μM (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15 cells)[2]. Seclidemstat (72 hours) mesylate promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434 cells)[2]. Seclidemstat (3 μM) mesylate promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line[2].

[1]. Dai XJ, et al. Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1 [published correction appears in J Med Chem. 2021 May 13;64(9):6410-6411]. J Med Chem. 2021;64(5):2466-2488.

[2]. Soldi R, et al. The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer. PLoS One. 2020;15(7):e0235705. Published 2020 Jul 10.