RN-1, LSD1 Inhibitor


Catalog No. size PriceQuantity
M60169-2D 10 mM DMSO (0.442 mL) $109
M60169-2S 2 mg solid $109
M60169-10S 10mg solid $441

Description

Product Information
Molecular Weight: 452.42
Formula: C23H29N3O2.2HCl
Purity: ≥98%
CAS#: 1221595-26-1
Solubility: DMSO up to 20 mM
Chemical Name: 2-(((1R,2S)-2-(4-(benzyloxy)phenyl)cyclopropyl)amino)-1-(4-methylpiperazin-1-yl)ethanone HCl salt
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

 

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

 

 


 

Products are for research use only. Not for human use.

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