RN-1 is a potent, specific and brain-penetrant Lysine Specific Demethylase-1 (LSD1) inhibitor. RN-1 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.
CAS Number: 1781835-13-9
Molecular Weight: 452.42
Related CAS Number:
1808255-63-1 (free base)
1221595-26-1 (free base rel)
1781835-13-9 (rel, 2HCl)
Chemical Name: 2-(((1R, 2S)-2-(4-(benzyloxy)phenyl)cyclopropyl)amino)-1-(4-methylpiperazin-1-yl)ethanone HCl salt, rel
Smiles: Cl.Cl.CN1CCN(CC1)C(=O)CN[C@@H]1C[C@H]1C1C=CC(=CC=1)OCC1C=CC=CC=1 |&1:13,15|
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO up to 20 mM
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
RN-1 was used at 1 µM in vitro.
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.
- Neelamegam R, et al. Brain-penetrant LSD1 inhibitors can block memory consolidation. (2012) ACS Chem Neurosci. 3(2):120-128.
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