RBC's HDAC assays and HAT assays can be used for the following:
-Larger scale HTS
-Large scale single dose, duplicate profiling
-IC50 profiling — 10 dose with curve fitting
-Custom Assay development
A variety of diseases are associated with dysfunction of the enzymes that add acetyl groups, histone acetyltransferases (HATs), and those that remove them, the HDACs (Histone Deacetylases, class I/II) and sirtuins (SIRTs, NAD+-dependent/class III HDACs). HDAC inhibitors have anti-proliferative effects on cancer cells and there are now two pan-HDAC inhibitors (HDACi’s), Vorinostat (SAHA) and Istodax (romidepsin) approved as drugs for cutaneous T-cell lymphoma (CTCL). Isoform-specific HDACi’s, targeting, for example, HDAC6, may represent the next wave in successful anti-cancer HDAC drug discovery. Aside from the well-known cancer example, possible indications for class I/II HDAC inhibitors include diabetes, high cholesterol, cardiac hypertrophy/inflammation, inflammatory bowel diseases and neurodegenerative disorders. Sirtuin activators are being pursued as a therapeutic strategy for diabetes, neurodegenerative disorders and aging-associated diseases in general. Inhibition of HATs is a potential route to therapies for neurodegeneration and chronic obstructive pulmonary disease (COPD).
RBC’s HAT assays are radioisotope-based filtration assays. This Gold Standard approach can be used regardless of whether the substrate is a peptide, histone, nucleosome or non-histone protein. With ~1750 lysine-acetylated proteins in the human proteome, RBC’s HAT Spectrum SM
assays provide an important advantage in terms of assay flexibility as well as 'Gold Standard' quality.
RBC's HDAC assays are fluorescent based.
**Certain HDAC assays performed under license from Cyclex Co Ltd.