Histone Acetyltransferase Assay (HAT) Services for Drug Discovery

Histone acetyltransferase assays performed at Reaction Biology are radiometric activity assays using tritiated acetyl-Coenzyme A as a cofactor.

Reaction Biology’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, Reaction Biology’s histone acetyltransferase assays provide an important advantage in terms of assay flexibility as well as gold standard quality.

  • Direct measurement of HAT activity
  • Low scale, large scale, and high-throughput HAT inhibitor screening options are available
  • Please ask us for HAT assay development and research collaboration options

List of HAT Activity Assays (7)

Target Synonyms Data
CPB CREBBP Data sheet
hGCN5 KAT2A Data sheet
KAT5 KAT5 Data sheet
MYST2 MYST2 Data sheet
MYST4 MYST4 Data sheet
p300 p300 Data sheet
pCAF KAT2B Data sheet

HAT Inhibitor Screening Details

Assay format
radiometric assay principle for histone acetylase screening of compounds for drug discovery based on acetylation of histones

Histone acetyltransferases acetylate lysines on histones and other proteins using tritium-labeled acetyl-Coenzyme A as the acetyl donor. The tritium-acetyl group is transferred onto the histone substrate that is measured directly to reflect the enzyme activity.

Assay setup

Setups: Single-dose screening in duplicates or IC50 value determination with 5 or 10 concentrations. Other screening formats are available upon request.

Controls: No inhibitor (DMSO vehicle) control and for every assay, one target-specific control compound is tested in 10-dose IC50 format. 

Turnaround time: 10 business days for standard projects. Expedited scheduling and data delivery can be arranged prior to the commencement of the studies.

Report: The raw data, % enzyme activity and control compound IC50 values will be reported in Excel format for single-dose assays. For IC50 orders, raw data, IC50 values, and curve fitting will be delivered in Excel format. Assay conditions, target, and substrate information are available upon request. Requirements for this information should be noted prior to the commencement of the study.

Screening facility: This assay is performed at our screening facility in Malvern, PA, US.

Compound requirements: In brief, for a standard project, 20 µl of a 10 mM DMSO stock or solid material is needed. Less material is needed for large scale screening. Please refer to our FAQs for information regarding compound preparation and shipping.