Lysine Acetyltransferase (KAT) Panel Screening Service

Diverse Enzyme Panel Selection for Broad Coverage

Our service begins with the careful selection of a comprehensive panel of recombinant KAT proteins. This panel includes key members from various families, such as the widely studied p300, the diverse MYST family (including MOF, MOZ, KAT6A/B, and KAT7), and the GCN5/PCAF group. These enzymes are often available with convenient FLAG tags, facilitating easy detection and purification for high-quality assay performance. This broad selection ensures that researchers can investigate a wide spectrum of KAT biology relevant to their specific research interests.

Advanced Assay Methodologies for Accurate Measurement

Creative Biolabs employs a suite of in-house developed biochemical assays meticulously optimized to measure KAT activity with high sensitivity and reliability. These assays typically utilize acetyl-CoA as the acetyl donor and monitor the acetylation of histone or peptide substrates. Our methodologies integrate various advanced techniques to ensure accurate quantification:

• Spectrophotometric and Fluorometric Assays: These methods rely on measuring changes in absorbance or fluorescence upon substrate acetylation. For instance, the detection of CoA release upon acetylation can be measured fluorometrically using thiol-sensitive fluorogenic probes like 7-diethylamino-3-(4'-maleimidylphenyl)-4-methylcoumarin (CPM). These assays offer an excellent balance of sensitivity, speed, and ease of use, making them ideal for high-throughput screening.
• Antibody-Dependent Assays: Utilizing highly specific antibodies that recognize acetylated lysine residues, these assays quantify the amount of antibody bound to the acetylated substrate. This approach is particularly valuable for studying the acetylation of specific lysine residues on proteins, providing precise insights into target modification.

While radioisotopic labeling provides high sensitivity, Creative Biolabs prioritizes non-radioactive methods for convenience and safety in our standard screening panels, ensuring efficient throughput without compromising data quality.

High-Throughput Inhibitor Screening and Potency Determination

A cornerstone of our service is the systematic screening of chemical libraries to identify potential KAT inhibitors. Our high-throughput screening capabilities allow for the rapid evaluation of thousands of compounds. Following initial hit identification, Creative Biolabs performs potency determination, typically calculating the half-maximal inhibitory concentration (IC50) for promising compounds. This quantitative measure is crucial for ranking the efficacy of potential drug candidates.

Rigorous Selectivity Profiling for Targeted Therapeutics

To assess the specificity of identified inhibitors, Creative Biolabs conducts rigorous selectivity profiling. This involves evaluating the effects of potential inhibitors across multiple KATs within the panel. Identifying compounds that selectively target specific KATs is paramount for developing therapeutics with minimal off-target effects, thereby improving drug safety and efficacy. Our detailed profiling helps researchers understand the precise inhibitory landscape of their compounds.

In-Depth Data Analysis and Expert Interpretation

At Creative Biolabs, we offer expert support for comprehensive data analysis and interpretation. Our proficient biological specialists analyze the results, identify significant hit compounds, and provide valuable insights into their potential mechanism of action. This expert guidance is critical for translating screening results into meaningful biological conclusions and informing subsequent research directions.

Strategic Follow-up Studies for Confirmatory Insights

Following initial screening, Creative Biolabs can provide further analysis to confirm findings and guide subsequent drug discovery efforts. This includes performing enzymatic assays using the same purified proteins to validate the observed effects and delve deeper into the kinetic properties of the enzyme-inhibitor interactions. These follow-up studies are designed to strengthen the evidence base and streamline the progression of promising candidates.