LSD1

Other Methylation Related Inhibitors

EZH2 PRMT MAT2A JMJD G9a/GLP SETD MLL COMT DOT1 HNMT

Cat.No.	Product Name	Information	Product Use Citations
S9734	Bomedemstat (IMG-7289)	Bomedemstat(IMG-7289) is an orally active and irreversible inhibitor of LSD1(lysine-specific demethylase 1). Bomedemstat exhibits the ability to enhance methylation levels of H3K4 and H3K9, subsequently leading to modifications in gene expression. Bomedemstat demonstrates anti-cancer properties by restraining cancer cell proliferation and prompting apoptosis.	Nat Commun, 2024, 15(1):7366
S6722	Seclidemstat (SP-2577)	Seclidemstat (SP-2577) is a potent and orally bioavailable inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A) with IC50 of 13 nM. This compound has potential antineoplastic activity.	bioRxiv, 2025, 2025.02.10.637435 Nat Commun, 2024, 15(1):5631 Nat Commun, 2023, 10.1038/s41467-023-42850-x
S9894	Vafidemstat	Vafidemstat(ORY-2001) is a potent, selective, brain-penetrant dual inhibitor of lysine-specific histone demethylase (LSD1, KDM1A) and MAO-B, with IC50 values of 105 nM and 58 nM, respectively. It shows potential for treating memory deficits and behavioral alterations in neurodegenerative and psychiatric diseases.
E4596	GSK-2879552	GSK-2879552 is a selective and potent inhibitor of Lysine-specific demethylase 1 (LSD1, KDM1A), with the potential to treat Small cell lung cancer (SCLC). It induces the expression of putative KDM1A target genes and demonstrates potent, predominantly cytostatic, antiproliferative activity in SCLC cell lines and tumor xenograft models.
E1899	INCB059872 dihydrochloride	INCB059872 dihydrochloride is a potent, selective, and irreversible inhibitor of Lysine-Specific Demethylase 1(LSD1). It exhibits potential antineoplastic activity and can be used in acute myeloid leukemia (AML) research.
S0356	Pulrodemstat (CC-90011) besylate	Pulrodemstat (CC-90011) besylate (LSD1-IN-7 benzenesulfonate) is a potent and orally active lysine specific demethylase-1 (LSD1) inhibitor that is found to be effective in various tumors.	Nat Commun, 2024, 15(1):7366
S8438	T-3775440 HCl	T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.	Cell Death Discov, 2024, 10(1):166
S7680	SP2509	SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. This compound induces apoptosis and promotes autophagy.	Cell Death Discov, 2025, 11(1):380 Cancer Res Commun, 2025, 5(9):1584-1598 bioRxiv, 2025, 2025.06.20.660795
S7796	GSK2879552 Dihydrochloride	GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with K_i_app of 1.7 μM. Phase 1.	EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2 EMBO Rep, 2025, 10.1038/s44319-025-00385-w Blood Adv, 2025, bloodadvances.2024015427
S7795	Ladademstat (ORY-1001) Dihydrochloride	ORY-1001 (RG-6016) 2HCl is an orally active and selective lysine-specific demethylase LSD1/KDM1A inhibitor with IC50 of <20 nM, with high selectivity against related FAD dependent aminoxidases. Phase 1.	EMBO Rep, 2025, 10.1038/s44319-025-00385-w Nat Commun, 2024, 15(1):5631 Cell Death Discov, 2024, 10(1):166