GSK-LSD1 Dihydrochloride

GSK-LSD1 Dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.

Signaling Pathways >> Epigenetics >> Histone Demethylase

Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase

Research Areas >> Cancer

IC50: 16 nM (LSD1)[1]

GSK-LSD1 Dihydrochloride shows more than 1000 fold selectivity over other closely related FAD utilizing enzymes including LSD2, and monoamine oxidases MAO-A, MAO-B[1]. GSK-LSD1 can inhibit KDM1A/LSD1 enzyme activity. GSK-LSD1 induces the formation of LC3-II in U2OS cells. The electronic microscopy shows the formation of autophagosome with GSK-LSD1 treatment. GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns[2].

[1]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215

[2]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.

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