cis-4-Br-2,5-F2-PCPA (S1024) inhibits LSD1 and LSD2 with Ki values of 94 nM and 8.4 μM, respectively. It inhibits LSD1 cell proliferation and increases dimethylated histone H3 at K4 (H3K4) in CCRF-CEM cells, particularly where there is aberrant expression of LSD1 in cancer stem cells [1].

cis-4-Br-2,5-F2-PCPA (compound 7c) effectively suppresses the proliferation of T-cell acute lymphoblastic leukemia (T-ALL) cells, with IC50 values of 12 µM for CCRF-CEM and 16 µM for Jurkat lines, while demonstrating no cytotoxic effects on the human normal fibroblast cell line WI-38. Additionally, at a concentration of 20 µM over a 24-hour period, it significantly enhances dimethylated H3K4 (H3K4me2) levels by 2.9 times compared to the control, indicating its role as a chemical inhibitor of LSD1 and LSD2 enzymes, as evidenced by Western Blot Analysis.