HDAC-6 Inhibitor Screening Kit
Rapid, simple, sensitive, and reliable fluorometric assay which is suitable for high throughput screening of HDAC6 inhibitors.
Histone Deacetylase 6 (HDAC-6, EC 220.127.116.11), is a class IIb HDAC enzyme that deacetylates an ε-N-acetyl lysine of histone and non-histone protein substrates. It is a unique member of HDAC family as it contains two deacetylase domains that are proposed to function independently of each other. HDAC-6 can shuttle between the nucleus and cytoplasm, suggesting potential extranuclear functions by regulating the acetylation status of non-histone substrates. HDAC-6 also affects transcription and translation by regulating the heat-shock protein 90 (Hsp90) and stress granules. Elevated HDAC-6 activity is associated with cell motility and catalyzes increases αtubulin deacetylation, thus influencing cancer cell metastasis. In addition, mutations in HDAC-6 gene have been associated with Alzheimer’s disease. HDAC6-selective inhibitors are considered as promising targets against autoimmune, inflammatory and oncology diseases such as breast and ovarian cancer.
The PromoKine HDAC-6 Inhibitor Screening Kit utilizes deacetylase activity of HDAC-6 towards a synthetic acetylated-peptide substrate resulting in the release of an AFC fluorophore, which can be easily quantified using a conventional microplate reader. In the presence of an HDAC-6-selective inhibitor (Tubacin), the deacetylase activity of HDAC-6 is reduced/abolished resulting in decrease or total loss of the fluorescence. This simple and high-throughput adaptable assay kit can be used to screen/study/characterize potential inhibitors of HDAC-6.