A cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50=5.27uM for hLSD1) and efficiently blocks LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50≤5uM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50≤5uM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50≤3.74uM). Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50≥100uM).
Synonyms:LSD Inhibitor III, Methyl-3-(4-(4-carbamimidoylbenzoyl)piperazine-1-carbonyl)-5-((4-carbamimidoylpiperazin-1-yl)methyl)benzoate, 3TFA, KDM1 Inhibitor III, Histone Lysine Demethylase Inhibitor V, BHC110 Inhibitor III
Formula:C₂₇H₃₄N₈O₄ • 3CF₃CO₂H
Solubility:DMSO
Molecular Weight:534.6
Storage and Stability:Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
