GSK2879552 2HCl

GSK2879552 2HCl (CAS No.: 1902123-72-1) is a synthetic small-molecule epigenetic modulator classified as a selective, irreversible inhibitor of lysine-specific demethylase 1 (LSD1/KDM1A), suitable for target validation, mechanistic elucidation, and lead compound evaluation in the context of biomedical research and drug discovery; as an antagonistic tool compound for FAD-dependent histone demethylases, it affects chromatin conformation and transcriptional networks by inhibiting the LSD1-mediated removal of H3K4 mono- and dimethylation, and is commonly used to investigate cell lineage differentiation, tumor-related transcriptional programs, and epigenetic dependencies. It exhibits low micromolar inhibitory activity in in vitro biochemical and cellular systems, with literature reporting an apparent inhibition constant Kiapp of approximately 1.7 μM; its irreversible binding property helps achieve sustained target occupancy and stable phenotypic readouts. This dihydrochloride form has been used in in vivo study designs with oral bioavailability characteristics and in pharmacokinetic/pharmacodynamic exploration, and has been used in oncology-related cellular and animal models to evaluate the effects of LSD1 inhibition on proliferation, differentiation, and transcriptional reprogramming; it can also serve as a control or probe compound in drug screening and combination-mechanism studies, used together with experimental approaches such as transcriptomic and epigenomic analyses, biomarker quantification, and functional phenotype assessment. The concentrations or doses used in experiments typically depend on the specific experimental design and research objectives, and should be optimized accordingly to ensure target specificity and reproducibility of the results.