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
Molecular Weight: 452.42. Empirical Formula: C23H29N3O2 · 2HCl. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 2. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51171514
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 489479-10MG