RN-1, LSD1 Inhibitor

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.

Product information

CAS Number: 1781835-13-9

Molecular Weight: 452.42

Formula: C23H31Cl2N3O2

Related CAS Number:

1808255-63-1 (free base)

1221595-26-1 (free base rel)

1781835-13-9 (rel, 2HCl)

1883545-53-6 (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|

InChiKey: WMHAFZOOUBPQRX-VSIGASKDSA-N

InChi: InChI=1S/C23H29N3O2.2ClH/c1-25-11-13-26(14-12-25)23(27)16-24-22-15-21(22)19-7-9-20(10-8-19)28-17-18-5-3-2-4-6-18;;/h2-10,21-22,24H,11-17H2,1H3;2*1H/t21-,22+;;/m0../s1

Technical Data

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

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.

References:

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.