S2157

S2157 is a selective, brain-permeable small molecule inhibitor of lysine-specific demethylase 1 (LSD1, also known as KDM1A), with an IC50 of 0.89 μM and >200-fold selectivity over related enzymes such as LSD2 and MAO-A. S2157 is a derivative of tranylcypromine and has demonstrated potent pharmacological effects against T-cell acute lymphoblastic leukemia (T-ALL) cells, primarily due to its LSD1 inhibition. While effective in vitro and in preclinical models, S2157 exhibits high hERG channel inhibition and poor microsomal metabolic stability, limiting its drug-likeness for clinical use[1][3][7]. Its mechanism offers potential as an epigenetic therapy targeting diseases where LSD1 contributes to pathogenesis, notably in some leukemias.