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).
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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
Recommended Products
Quality Level
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
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
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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