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10010494 2-PCPA (hydrochloride)
trans-2-Phenylcyclopropylamine (hydrochloride); Tranylcypromine (hydrochloride)
2-PCPA (hydrochloride) Workbook Links
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Histones contain unstructured N-terminal residues that are the site of numerous post-translational modifications, involving acetylation, methylation, ubiquitination, and sumoylation to produce a specific gene regulatory outcome.1 Complementary enzymes catalyze the addition and removal of these modifications as needed. The amine oxidase domain-containing enzyme lysine-specific demethylase 1 (LSD1) is a member of one of two classes of histone demethylases capable of demethylating lysine residues.1 LSD1 shares similar catalytic sites with monoamine oxidases (MAO) A and B, the inhibition of which are used clinically to treat depression, anxiety, and Parkinson · s disease.2 2-PCPA is an irreversible, mechanism-based inhibitor of LSD1 with an IC50 value of 20.7 µM and a Ki value of 242.7 µM that effectively inhibits histone demethylation in vivo.3 Although not as selective, 2-PCPA also irreversibly inhibits MAO A and MAO B with IC50 values of 2.3 and 0.95 µM and Ki values of 101.9 and 16 µM, respectively.3
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1
Forneris, F., Binda, C., Vanoni, M.A., et al. Human histone demethylase LSD1 reads the histone code. J Biol Chem 280(50) 41360-41365 (2005).
2
Lee, M.G., Wynder, C., Schidt, D.M., et al. Histone H3 lysine 4 demethylation is a target of nonselective antidepressive medications. Chemistry & Biology 13 563-567 (2006).
3
Schmidt, D.M.Z., McCafferty, D.G. trans-2-Phenylcyclopropylamine is a mechanism-based inactivator of the histone demethylase LSD1. Biochemistry 46 4408-4416 (2007).
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Purchase 10010494 2-PCPA (hydrochloride)
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This product is also available to buy in bulk quantities.
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Warning This product is not for human or veterinary use.
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Pricing updated 2010-03-15.
Prices are subject to change without notice.
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