货号 | 18124-1mg |
描述 | Lysine-specific demethylase 1 (LSD1) belongs to the family of flavin adenine dinucleotide (FAD)-dependent amine oxidases that include monoamine oxidases (MAOs).1 RN-1 is a potent, irreversible inhibitor of LSD1 (IC50 = 70 nM).2 It is much less effective against MAO-A and MAO-B (IC50s = 0.51 and 2.8 µM, respectively).2 Following intraperitoneal administration, RN-1 penetrates the blood-brain barrier and distributes in mice to a brain/plasma exposure ratio of 88.9.2 It blocks long-term but not short-term memory in mice.2 RN-1 also induces cytotoxicity in ovarian cancer cell lines and induces fetal hemoglobin synthesis while reducing disease pathology in sickle cell mice.3,4 |
别名 | LSD1 Inhibitor IV; |
供应商 | Cayman |
应用文献 | |
1.Shi, Y.,Lan, F.,Matson, C., et al. Histone demethylation mediated by the nuclear amine oxidase homolog LSD1. Cell 119, 941-953 (2004). 2.Neelamegam, R.,Ricq, E.L.,Malvaez, M., et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. ACS Chem.Neurosci. 3, 120-128 (2012). 3.Konovalov, S., and Garcia-Bassets, I. Analysis of the levels of lysine-specific demethylase 1 (LSD1) mRNA in human ovarian tumors and the effects of chemical LSD1 inhibitors in ovarian cancer cell lines. J.Ovarian Res. 6(1), 75 (2013). 4.Cui, S.,Lim, K.C.,Shi, L., et al. The LSD1 inhibitor RN-1 induces fetal hemoglobin synthesis and reduces disease pathology in sickle cell mice. Blood 126(3), 286-296 (2015). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 452.4 |
分子式 | C23H29N3O2 • 2HCl |
CAS号 | 1781835-13-9 |
稳定性 | ≥ 2 years |
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