| 产品介绍 |
HCI-2509 (also named as SP2509 or LSD1-C12) is a highly potent, specific, and reversible Lysine Specific Demethylase-1 (LSD1) inhibitor. It inhibits LSD1 in biochemical assay with an IC50 ~13 nM, and has no activity against monoamine oxidase proteins MAO-A and MAO-B (>300 μM). HCI-2509 is a non-competitive inhibitor to bind LSD1, changes its solution dynamics in a manner distinct from TCP. It has minimal inhibition of CYPs and hERG, shows cellular activity against several cancer cell lines including endometrial, breast, colorectal, pancreatic, and prostate cancer (IC50 ~0.3-2.5 μM). HCI-2509 displayed sing-agent efficacy in multiple xenograft models and had good PK/PD relationship by using tumor histone H3K4 and H3K9 methylation. HCI-2509 serves as a very useful chemical probe to study the target biology of LSD1.
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