A Selective Phenelzine Analogue Inhibitor of Histone Demethylase LSD1 was written by Prusevich, Polina;Kalin, Jay H.;Ming, Shonoi A.;Basso, Manuela;Givens, Jeffrey;Li, Xin;Hu, Jianfei;Taylor, Martin S.;Cieniewicz, Anne M.;Hsiao, Po-Yuan;Huang, Rong;Roberson, Heather;Adejola, Nkosi;Avery, Lindsay B.;Casero, Robert A. Jr.;Taverna, Sean D.;Qian, Jiang;Tackett, Alan J.;Ratan, Rajiv R.;McDonald, Oliver G.;Feinberg, Andrew P.;Cole, Philip A.. And the article was included in ACS Chemical Biology in 2014.Safety of 1-(3-Bromopropyl)-4-methoxybenzene This article mentions the following:
Lysine-specific demethylase 1 (LSD1) is an epigenetic enzyme that oxidatively cleaves Me groups from monomethyl and di-Me Lys 4 of histone H3 (H3K4Me1, H3K4Me2) and can contribute to gene silencing. This study describes the design and synthesis of analogs of a monoamine oxidase antidepressant, phenelzine, and their LSD1 inhibitory properties. A novel phenelzine analog (bizine) containing a phenyl-butyrylamide appendage was shown to be a potent LSD1 inhibitor in vitro and was selective vs. monoamine oxidases A/B and the LSD1 homolog, LSD2. Bizine was found to be effective at modulating bulk histone methylation in cancer cells, and ChIP-seq experiments revealed a statistically significant overlap in the H3K4 methylation pattern of genes affected by bizine and those altered in LSD1-/- cells. Treatment of two cancer cell lines, LNCaP and H460, with bizine conferred a reduction in proliferation rate, and bizine showed additive to synergistic effects on cell growth when used in combination with two out of five HDAC inhibitors tested. Moreover, neurons exposed to oxidative stress were protected by the presence of bizine, suggesting potential applications in neurodegenerative disease. In the experiment, the researchers used many compounds, for example, 1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3Safety of 1-(3-Bromopropyl)-4-methoxybenzene).
1-(3-Bromopropyl)-4-methoxybenzene (cas: 57293-19-3) belongs to organobromine compounds. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Safety of 1-(3-Bromopropyl)-4-methoxybenzene
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary