INCB059872 is a highly potent, orally active, selective, and irreversible inhibitor of Lysine-Specific Demethylase 1 (LSD1). Its chemical properties make it suitable for use in researching myeloid leukemia.

INCB059872 (25 nM; 48 hours; 293T cells) upregulates enhancer activity and gene expression[1]. INCB059872 (25 nM; 24 hours; THP-1 cells) induces a growth defect in THP-1 cells within one doubling time (approximately 3 days). In MV-4-11 cells, INCB059872 (100 nM; 24 hours) does not impede growth similarly to DMSO-treated cells. INCB059872 (THP-1 cells) regulates genes and enhancers as identified by PRO-seq analysis[1]. Western Blot Analysis in 293T cells (250 nM; 48 hours) shows increased enhancer activity and gene expression.

Administering INCB059872 (10 mg/kg; p.o.; 0, 4, or 6 days) in mice altered bone marrow progenitor populations, as identified by single-cell RNA sequencing[1].