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RN-1 is a potent, specific and brain-penetrant Lysine Specific Demethylase-1 (LSD1) inhibitor. It inhibits LSD1 in biochemical assay with an IC₅₀ ~70 nM, and has weaker activity against monoamine oxidase proteins MAO-A and MAO-B with IC₅₀ ~0.51 μM and 2.79 μM respectively. It exhibits good brain penetration and retention following systemic administration. RN-1 can abolish long-term memory formation without affecting short-term memory in the novel object recognition (NOR) mouse model. RN-1 could be a useful chemical probe to study the importance of reversible histone methylation in the function of the nervous system.

How to Use:

• In vitro: RN-1 was used at 1 μM in vitro.
• In vivo: RN-1 was administered by intraperitoneal injection once a day at a dose of 10-30 mg/kg to the novel object recognition (NOR) mouse model. RN-1 exhibits good brain penetration and retention.

Reference:

1. 1. Neelamegam R, et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. (2012) ACS Chem Neurosci. 3(2):120-128.

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