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S2101 (also known as LSD1 Inhibitor II) is a selective, cell-permeable, small-molecule irreversible inhibitor of lysine-specific demethylase 1A (KDM1A/LSD1). Developed by researchers at RIKEN and Nagoya City University, S2101 is a derivative of trans-2-phenylcyclopropylamine (2-PCPA) designed to exhibit enhanced potency and selectivity for LSD1 over monoamine oxidases A and B (MAO-A and MAO-B). It exerts its inhibitory effect by forming a covalent adduct with the flavin adenine dinucleotide (FAD) cofactor of LSD1. S2101 is widely utilized as a chemical biology research tool to investigate the role of epigenetic regulation in cancer stem cell maintenance, cellular differentiation, and viral reactivation, particularly in models of leukemia, glioblastoma, and ovarian cancer.
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