Histone Deacetylase 5 or HDAC-5 belongs to Class II Histone deacetylase family. It represses transcription by deacetylating lysine residues on the N-terminal part of histones H2A, H2B, H3 and H4. This epigenetic repression caused by HDAC-5, plays a role in transcriptional regulation, cell cycle progression and development. It interacts with myocyte enhancing factor (MEF-2) proteins that are associated with colon cancer, causing the repression of MEF-2 dependent gene expression. HDAC-5 is also involved in epigenetic regulation of ESR1 expression in breast cancer. HDAC-5 inhibition induces reactive oxygen species (ROS) production, ultimately leading to apoptotic cell death as well as mechanisms of mitochondrial quality control processes such as mitophagy and mitobiogenesis. Therefore, HDAC-5 inhibition in cancer cells significantly reduces tumor size due to apoptotic cell death of cancer cells (Hendrick, et al, Oncogene. 2017 Aug 24, 36(34):4859-4874), which makes HDAC-5 an attractive target for anti-cancer therapy. BioVision’s HDAC-5 Inhibitor Screening Kit is a plate-based fluorometric kit for screening potential HDAC-5 inhibitors. The principle of the kit is based on the deacetylation of an acetylated substrate by HDAC-5. The deacetylated product is then cleaved by a developer to release a highly fluorescent moiety with Ex/Em= 380/460 nm. Trichostatin A, a well-known HDAC inhibitor is provided as inhibitor control.
Biochemical and cellular assays