Cat No:LP000319
Product Name:SP2509;HCI-2509;LSD1 Inhibitor VII
Molecular Formula:C19H20ClN3O5S
Molecular Weight:437.90
Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4), resulting in transcriptional repression.1 SP2509 is a reversible inhibitor of LSD1 (IC50 = 13 nM).2 It has no effect on monoamine oxidases A and B. SP2509 attenuates the binding of LSD1 to CoREST, allowing increased methylation of H3K4 and driving increased expression of p21, p27, and CCAAT/enhancer binding protein α in cultured acute myeloid leukemia (AML) cells.2,3 It improves survival of mice with AML xenografts when given (25 mg/kg biweekly via intraperitoneal injection) for three weeks.2 Co-treatment of SP2509 with the pan-HDAC inhibitor panobinostat (Item No. 13280) synergistically kills AML cells in vitro and improves survival of mice engrafted with AML cells.

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