Stemcell, 100-1643, SP2509

Inhibit cell growth and induce apoptosis in cancer cells with SP2509, a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1; IC50 = 13 nM). LSD1, also known as KDM1A, demethylates mono- and di-methylated lysine residues on histone H3 to regulate transcription and is a key component of the Mi-2/nucleosome remodeling and deacetylase (NuRD) complex that has been implicated in many cancers (Hayami et al. Int J Cancer, 2011; Sorna et al. J Med Chem, 2013). By inhibiting LSD1, SP2509 disrupts the formation of complexes that regulate expression of genes related to cell growth and apoptosis in cancer cells (Sankar et al. Clin Cancer Res, 2014).

SP2509 has been used for:

CANCER RESEARCH

· Induce apoptosis in human Ewing sarcoma cell lines and reduce tumor growth in an Ewing sarcoma mouse xenograft model (Sankar et al. Clin Cancer Res, 2014).

· Downregulate Bcl-2 and Mcl-1 expression to induce apoptosis in human renal carcinoma cells (Wu et al. J Cancer Prev, 2020).

· Inhibit cell growth and apoptosis in human lung cancer cell lines and in vivo in a mouse xenograft model (Zhen et al. Acta Biochim Biophys Sin, 2021).

· Induce apoptosis, reduce colony formation, promote differentiation of human acute myeloid leukemia (AML) cells, and improve survival in an AML mouse xenograft model (Fiskus et al. Leukemia, 2014).