1357302-64-7

Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4) and H3K9, resulting in transcriptional repression. Host LSD1 is also recruited by certain viruses to limit H3K9 methylation, which can repress viral genes necessary for infection. Lysine-specific demethylase 1 (LSD1) is a protein lysine demethylase that specifically demethylates histone H3 lysine 4 (H3K4) and H3K9, resulting in transcriptional repression. Host LSD1 is also recruited by certain viruses to limit H3K9 methylation, which can repress viral genes necessary for infection. OG-L002 is a potent inhibitor of LSD1 (IC₅₀ = 0.02 μM) that less effectively inhibits the monoamine oxidases A (MAO-A) and MAO-B (IC₅₀s = 1.38 and 0.72 μM). It blocks the expression of immediate early (IE) genes of herpes simplex virus (HSV) in HeLa cells but not that of cellular control genes. OG-L002 also reduces the expression of human cytomegalovirus IE genes and adenovirus E1A gene in mammalian cells. It is effective in vivo, repressing HSV primary infection in mice and blocking HSV reactivation from latency in a mouse ganglion explant model.

OG-L002 is a novel, potent, and selective LSD1/KDM1A inhibitor that epigenetically blocks the herpes simplex lytic replication and reactivation from latency.

This histone H3K9 demethylase inhibitor (FW = 669.82 g/mol; CAS 1357302-64-7; Solubility: 45 mg/mL DMSO; <1 mg/mL H2O) potently and specifically inhibits the histone demethylase LSD1 (IC50 = 20 nM), resulting in increased repressive chromatin assembly and suppression of gene expression during the lytic phase of herpes simplex virus and varicella-zoster virus infection. This LSD1 inhibitor also blocks initial gene expression of the human cytomegalovirus and adenovirus type 5, attesting to the critical role of LSD1 in regulating DNA virus infection. Because this small-molecule inhibitor was originally designed to inhibit monoamine oxidases, it is noteworthy that its affinity for LSD1 is 36x and 69x higher than MAO-B and MAO-A, respectively.

LSD1

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[1] FEDERICO FORNERIS. Human histone demethylase LSD1 reads the histone code.[J]. The Journal of Biological Chemistry, 2005, 280 50: 41360-41365. DOI: 10.1074/jbc.m509549200
[2] YU LIANG. A novel selective LSD1/KDM1A inhibitor epigenetically blocks herpes simplex virus lytic replication and reactivation from latency.[J]. mBio, 2013, 4 1: e00558-12. DOI: 10.1128/mbio.00558-12