Inhibiteur LSD1 IV;RN-1 ; HCl

Non disponible en dehors du Royaume-Uni et de l'Irlande

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.).

Legal Information

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

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)