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GSK LSD1 Dihydrochloride is an irreversible mechanism-based inhibitor of LSD1. Lysine-specific demthylase 1 (LSD1) belonges to the flavin adenine dinucleotide (FAD) family-dependant amine oxidases that include MAOs and PAOs. Inhibits cell proliferation in cancer cell lines.

GSK-LSD1 has been used as a lysine specific demethylase 1 (LSD1) inhibitor in mice to study sepsis-induced mortality. It has also been used as an inhibitor to study if the effect of phenelzine activation of human immunodeficiency virus (HIV) latency is caused due to LSD1.

gsk-lsd1 2hcl is a selective inhibitor of lsd1 with ic50 value of 16 nm [1].lysine (k) -specific demethylase 1a (lsd1) is a flavin-dependent histone demethylase that demethylates mono- and di-methylated lysines and plays an important role in oocyte growth, embryogenesis and tissue-specific differentiation. lsd1 plays a role in acute myeloid leukemia (aml).gsk-lsd1 2hcl irreversibly inhibited lsd1 with ic50 value of 16 nm and is > 1000 fold selective over lsd2, mao-a and mao-b, which were related to fad utilizing enzymes. in cancer cell lines, gsk-lsd1 2hcl changed gene expression with average ec50 value < 5 nm and inhibited cells growth with average ec50 value < 5 nm. gsk-lsd1 2hcl (10 ?m) inhibited human recombinant dopamine transporter, 5-ht1a and 5-ht transporter by 39%, 49% and 74%, respectively. and no activity against other 55 recombinant receptors (gpcr, transporters, ion channels). gsk-lsd1 2hcl can be used as a chemical probe and a part of the sgc epigenetics [1].

GSK-LSD1 is a potent and selective inhibitor of lysine specific demethylase 1 (LSD1). GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns. For full characterization details, please visit the GSK-LSD1 probe summary on the Structural Genomics Consortium (SGC) website.To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

[1]. structural genomics consortium.http://www. thesgc.org/chemical-probes/lsd1.