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GSK-LSD1 is a highly potent, specific and irreversible inhibitor of Lysine Specific Demethylase-1 (LSD1). It inhibits LSD1 in biochemical assay with an IC₅₀ ~16 nM, and is > 1000 fold selective over other closely related FAD utilizing enzymes (i.e. LSD2, MAO-A, MAO-B).  GSK-LSD1 induces gene expression changes in cancer cell lines (average EC50 < 5 nM) and inhibits cancer cell line growth (average EC50 < 5 nM). 

How to Use:

• In vitro:  GSK-LSD1 was used at 1 µM in vitro.
• In vivo:  n/a

Reference:

• 1. http://www.thesgc.org/chemical-probes/epigenetics