INCB059872

INCB059872 is a potent, orally active, selective and irreversible Lysine-Specific Demethylase 1 (LSD1) inhibitor. INCB059872 can be used for the research of myeloid leukemia[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Demethylase

LSD1[1]

INCB059872 (25 nM; 48 hours; 293T cells) increases enhancer activity and gene expression[1]. INCB059872 (25 nM; 24 hours; THP-1 cells) makes THP-1 show a growth defect within one cell doubling time or approximately 3 days. INCB059872 (100 nM; 24 hours; MV-4–11 cells) treated MV-4–11 cells continues to grow as DMSO-treated cells for multiple cell divisions. INCB059872 (THP-1 cells) regulates PRO-seq analysis identifies genes and enhancers[1]. Western Blot Analysis[1] Cell Line: 293T cells Concentration: 250 nM Incubation Time: 48 hours Result: Increased enhancer activity and gene expression.

INCB059872 (10 mg/kg; p.o.; 0, 4, or 6 days) makes single-cell RNA-seq revealing changes in bone marrow progenitor populations[1]. Animal Model: Mice[1] Dosage: 10 mg/kg Administration: P.o.; 0, 4, or 6 days Result: Single-cell RNA-seq revealed changes in bone marrow progenitor populations.

[1]. Johnston G, et al. Nascent transcript and single-cell RNA-seq analysis defines the mechanism of action of the LSD1 inhibitor INCB059872 in myeloid leukemia. Gene. 2020;752:144758.