FLUOR DE LYS^® HDAC1 fluorometric drug discovery assay kit

• Useful for inhibitor screening or characterizing enzyme kinetics
• Includes optimal substrate selected from a panel of acetylated sites in p53 and histones
• Supplied with enough recombinant enzyme for 96 assays (1 x 96-well plate)

A FLUOR DE LYS^® fluorescent assay system. The HDAC1 Fluorescent Activity Assay/Drug Discovery Kit is a complete assay system designed to measure the lysyl deacetylase activity of the recombinant human HDAC1 included in the kit. The kit is ideal for chemical library screening for candidate inhibitors or kinetic assay of the enzyme under varying conditions. The FLUOR DE LYS^® HDAC1 assay is based on the FLUOR DE LYS^® Substrate and FLUOR DE LYS^® Developer combination. The assay procedure has two steps. First, the FLUOR DE LYS^® Substrate, which comprises an acetylated lysine side chain, is incubated with HDAC1. Deacetylation of the substrate sensitizes the substrate so that, in the second step, treatment with the FLUOR DE LYS^®Developer produces a fluorophore.

Human HDAC1 (HD1) was the first protein to be linked to histone deacetylase activity. It is homologous to the yeast protein Rpd3, a relationship which has since come to define the “class I HDACs”. HDAC1 promotes transcriptional repression by deacetylating lysine ε-amino groups in histone N-terminal tails, a function frequently carried out in association with multi-protein transcription repression complexes such as NuRD, Sin3> and CoREST. Ubiquitously expressed in human tissues, HDAC1-containing complexes appear to contribute the greater part of (at least class I) deacetylase activity in HeLa nuclear extracts. Aside from its interaction with co-repressors, HDAC1 activity may be regulated by post-translation modifications such as phosphorylation and sumoylation or binding to the inhibitor maspin, a tumor-suppressive serpin homolog. Although originally described as a “histone deacetylase”, HDAC1 has been shown to catalyze the regulatory deacetylation of non-histone proteins, including p53. Overexpression of HDAC1 has been found in various cancer types. HDAC inhibitors (HDACi) have shown considerable promise as anti-cancer agents and HDACi compounds from multiple chemical classes are in stages of drug development ranging from preclinical to phase III trials. HDAC inhibitors have shown promise as anti-tumor agents and naturally this has stimulated interest in the screening of compounds for HDAC1 inhibition.