CBB1007 trihydrochloride is a cell-permeable, potent, reversible and substrate competitive (LSD1, KDM1A) selective inhibitor with IC50 of 5.27 uM.
CBB1007 efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities.
CBB1007 induces activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM).
CBB1007 preferentially arrests the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cell.
