Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4), resulting in transcriptional repression.{14724} SP2509 is a reversible inhibitor of LSD1 (IC50 = 13 nM).{28684} 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.{28684,28685} It improves survival of mice with AML xenografts when given (25 mg/kg biweekly via intraperitoneal injection) for three weeks.{28684} 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.{28684,28685}
產品描述
A reversible inhibitor of LSD1 (IC50 = 13 nM); allows increased methylation of H3K4, driving increased expression of p21, p27 and CCAAT/enhancer binding protein α in cultured AML cells; improves survival alone and synergizes with panobinostat in improving survival of mice engrafted with AML cells
