Cat.No.: | EKIT-0589 |
Product Name: | LSD1 fluorometric drug discovery kit |
Size: | 96 reactions |
Product Overview: | Fluorescent detection, HTS, Activity assay, Cell-based assays |
Description: | 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) 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. 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. |
Background: | 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. |
Kit Components: | Recombinant human LSD1 (50µg, >1000U)Histone H3 Dimethyl Lysine-4 Peptide SubstrateCELLESTIAL Red Peroxidase SubstrateHorseradish PeroxidaseH2O2 StandardTranylcypromine (LSD1 inhibitor)Black and clear 1/2-vol. 96-well platesDetailed instructions |
Storage: | -80°C |
Warning: | For research use only, not for diagnostic use. |
Product Types | ||
◆ Research Kits | ||
EKIT-0062 | Histone Demethylase LSD1 Activity/Inhibition Assay Kit | Inquiry |
EKIT-0126 | LSD1 Inhibitor Screening Assay Kit | Inquiry |
EKIT-0160 | LSD1 Demethylase Activity/Inhibition Fluorometric Assay Kit | Inquiry |
◆ Bioactive Small Molecules | ||
BSM-0111 | DDP-38003 dihydrochloride | Inquiry |
BSM-0141 | GSK-LSD1 dihydrochloride | Inquiry |
Related Gene / Proteins | |||
LSD1 | LSD2 | LSM2 | LSM3 |
LSM5 | LSM6 | LSP1 |
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