489479

LSD1 Inhibitor IV, RN-1, 2HCl

LSD1 Inhibitor IV, RN-1, HCl, is a cell-permeable potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC₅₀ = 70 nM in a HRP-coupled assay using H3K4Me2 peptide substrate).

• Synonym(s): LSD1 Inhibitor IV, RN-1, 2HCl, LSD Inhibitor IV, Histone Lysine Demethylase Inhibitor VI, MOA Inhibitor III, 2-(1R,2S)-2-(4-(Benzyloxy)phenyl)cyclopropylamino)-1-(4-methylpiperazin-1-yl)ethanone, HCl, BHC110 Inhibitor IV, KDM1 Inhibitor IV, LSD Inhibitor IV, KDM1 Inhibitor IV, Histone Lysine Demethylase Inhibitor VI, MOA Inhibitor III, 2-(1R,2S)-2-(4-(Benzyloxy)phenyl)cyclopropylamino)-1-(4-methylpiperazin-1-yl)ethanone, HCl, BHC110 Inhibitor IV
• Empirical Formula (Hill Notation): C₂₃H₂₉N₃O₂ · 2HCl
• Molecular Weight: 452.42
• UNSPSC Code: 12352208
• NACRES: NA.28

Properties

• Quality Level: 200
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; desiccated (hygroscopic); protect from light
• color: yellow
• solubility: DMSO: 2.5 mg/mL; water: 2.5 mg/mL
• shipped in: wet ice
• storage temp.: −20°C

Description

General description

A cell-permeable tranylcypromine (parnate; Cat. No. 616431) analog that acts as a potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC₅₀ = 70 nM in a HRP-coupled assay using H3K4Me2 peptide substrate). Forms a covalent adduct with flavin adenine dinucleotide (FAD). Shown to cross the blood brain barrier. Exhibits moderate selectivity over amine oxidases MAO-A and MAO-B (IC₅₀ = 0.51 and 2.785 µM, respectively). Displays desirable pharmacokinetic properties (brain/plasma exposure ratio of 88.9), and impairs long-term memory without affecting short-term memory in mice (10 mg/kg, i.p.).

A cell-permeable tranylcypromine (parnate; Cat. No. 616431) analog that acts as a potent, irreversible inhibitor of lysine specific demethylase 1 (LSD1; IC₅₀ = 70 nM in a HRP-coupled assay using H3K4Me2 peptide substrate). Forms a covalent adduct with flavin adenine dinucleotide (FAD). Shown to cross the blood brain barrier. Exhibits moderate selectivity over amine oxidases MAO-A and MAO-B (IC₅₀ = 0.51 and 2.785 µM, respectively). Displays desirable pharmacokinetic properties (brain/plasma exposure ratio of 88.9), and impairs long-term memory without affecting short-term memory in mice (10 mg/kg, i.p.).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Neelamegam, R., et al. 2011. ACS Chem. Neurosci.3, 120.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable