LSD1 fluorometric drug discovery kit

The LSD1 Fluorimetric Drug Discovery Kit provides human recombinant LSD1 and all reagents for measuring its activity in a sensitive, real-time fluorescent assay. LSD1 catalyzed demethylation of the Histone H3 Dimethyl Lysine-4 Peptide (H3K4Me2 Peptide; Prod. No. BML-P256) produces hydrogen peroxide. A fluorescent signal is generated via the horseradish peroxidase (HRP) catalyzed reaction of the hydrogen peroxide with the CELLESTIAL^® Red Peroxidase Substrate (Prod. No. BML-KI565). Although fluorescence detection will be more sensitive (Excitation in range of 530-570 nm; Emission ca. 590 nm), the CELLESTIAL^® Red peroxidation product may also be detected by following absorbance (see “Detection by Absorbance at 563 nm”).

LSD1 (aka KDM1; lysine-specific histone demethylase 1; AOF2), a flavin-containing amine oxidase homolog and component of various corepressor complexes, was the first enzyme demonstrated to be capable of lysine demethylation1. LSD1 catalyzes the oxidative demethylation of mono- and dimethylated histone 3 lysine-4 (H3K4Me2/1), producing hydrogen peroxide and formaldehyde in the process. H3K4 methylation is considered a transcription-activating chromatin mark and, in vivo, LSD1 is frequently found in association with the transcriptional corepressor protein CoREST and HDACs 1 or 23. LSD1 is inhibited by a number of established monoamine oxidase inhibitor drugs, including tranylcypromine. That and the fact that its expression is elevated in a number of cancers may make it a promising target for drug development.