Epigenetic Proteins Product Solutions

Epigenetics involves the study of heritable or acquired changes in gene expression caused by non-genetic mechanisms without alterations in gene structure or sequence. Basic epigenetic mechanisms such as histone modifications, DNA methylation, and chromatin remodeling are essential in the regulation of many physiological processes. Alterations to the mechanisms -- either by modifications to DNA and histone components of nucleosomes, or by expression of noncoding RNAs (ncRNAs) -- can have implications in a number of cancers, immunological, and neurodegenerative conditions.


Eurofins DiscoverX® offers epigenetics recombinant proteins and InCELL Hunter™ cell-based assays for studying the modulation of epigenetic mechanisms and identifying small molecule inhibitors and modifiers of DNA methyltransferases and bromodomains. Utilize InCELL Hunter cell-based compound-target engagement assays to confirm small molecule compound cell entry and epigenetic target binding, screen and rank inhibitors, validate hits identified in biochemical assays, and measure cellular EC50 values all in the native cellular environment.

Product Highlights

  • Biologically Relevant - Obtain quantitative cellular compound entry and epigenetic target binding data for more confident drug discovery decisions
  • Easy-to-use & Scalable - Simple, homogeneous, and high-throughput amenable protocol to easily measure compound binding to your epigenetic target with a chemiluminescent readout
  • Target Specificity & Selectivity - Ability to screen and differentiate multiple target-selective stereoisomers of BRD4 and determine target specificity
  • High Quality Proteins - Access epigenetics-related recombinant proteins produced using optimal expression systems with high quality and purity
Consider Eurofins DiscoverX’s custom development capabilities for custom cell lines, assays, & enzyme development.
  • Epigenetic Proteins – Recombinant epigenetic proteins, expressed in E. coli and tagged (e.g. GST, His6), and used in EPIscan screening and profiling services
  • InCELL Hunter Epigenetic Cell Lines – Stable cell lines confirmed for past 10 passages and rigorously and continuously validated for accurate pharmacology through Eurofins Discovery services with billions of data points screened.
  • InCELL Hunter eXpress Kits – Complete assay-ready kits with specific cell line, optimized reagents, and plates for quick Enzyme Fragment Complementation (EFC) based chemiluminescent detection.
  • InCELL Pulse Starter Kit – Create your own cell-based, target engagement assays with reagents and protocol for the design and development of InCELL Pulse assays for the measurement of inhibitor cellular potency against user-defined epigenetic targets of interest.
  • InCELL Detection Kit – Measure compound binding to a specific protein target in InCELL Hunter and InCELL Pulse cell lines

InCELL Hunter Assay Principle

InCELL Hunter stabilization assays are based on the industry validated Enzyme Fragment Complementation (EFC) technology and built on the principle of protein stabilization related to the protein turnover. Cells expressing a protein of interest is fused to the small EFC enzyme donor of β-galactosidase (β-gal) called ePL (enhanced ProLabel®). Upon addition of When a compound that binds the target is applied, protein levels are stabilized or altered in the cell, and this change can be monitored by measuring target protein abundance using chemiluminescent detection. Upon addition of the large EFC enzyme acceptor (EA) fragment and chemiluminescent substrate, EA naturally complements with the ePL tag on the target protein to create an active β-gal enzyme. The resulting active enzyme hydrolyzes the substrate to generate a chemiluminescent signal. The greater the signal, the greater the amount of stabilized target protein, and thus the greater the presence of compound-target engagement in the cell.

InCELL Pulse Assay Principle

InCELL Pulse™ compound-target engagement assays are based on the EFC technology incorporating compound binding detection based on protein thermal stability. Cells expressing a protein of interest is fused to the small EFC β-gal enzyme donor ePL. These cells are treated with test compound and then subjected to elevated temperatures during a pulse denaturation step. The larger EFC enzyme donor (EA) of β-gal is then added with a chemiluminescnent substrate and EFC complementation is allowed to occur. Compound binding protects the target protein from thermal denaturation, which enhances complementation between added the EA and ePL components and increases the chemiluminescent signal measured using the EFC-based detection system.

Scientific Posters InCELL Pulse: Cellular Target Engagement Assay Platform for Drug Discovery

It is well established that ligand binding can protect proteins from thermal denaturation in a cellular milieu; however, the broad…

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Scientific Posters InCELL Hunter™: A Novel Cellular Assay Platform for the Direct Measurement of Compound Binding to Intracellular Targets in Intact Mammalian Cells

Assays that directly detect compound binding inside cells can be of great utility in translating in vitro data to more…

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Scientific Posters Mix-and-Read Assays For Regulated Ubiquitination & Degradation of Proteins Using PathHunter® Technology

Ubiquitin-mediated degradation of signaling proteins is a primary means of signal regulation in a wide variety of cellular processes including…

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Webinars Create Your Own Cellular Compound Target Engagement Assay

Here we will describe InCELL Pulse™, which uses DiscoverX’s Enzyme Fragment Complementation (EFC) technology to overcome these limitations of current…

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Webinars Creating Cellular Target Engagement Assays for Diverse Kinases Using InCELL Pulse

Kinase inhibitors often potently inhibit several off-target kinases in biochemical assays. Unfortunately, the relevance of these off-target interactions in a…

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Webinars Create Your Own InCELL Pulse Cellular Compound Target Engagement Assay

It is well established that ligand binding can protect proteins from thermal denaturation in a cellular milieu; however, the broad…

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Videos InCELL Compound-Target Engagement Assays for Drug Discovery

Learn how InCELL cell-based binding assays can be used to detect compound cell entry and engagement to specific targets including…

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Videos Custom Development Capabilities

Learn about Eurofins DiscoverX cell line engineering, assay development, and recombinant enzyme production custom capabilities. Find out more about cell…

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Blogs & Articles Enabling High-Throughput Screening for Cellular Compound-Target Engagement

Information on compound-target engagement obtained from traditional in vitro binding assays differs greatly from that in a physiologically relevant model…

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Blogs & Articles Comparison of InCELL Hunter™ vs InCELL Pulse™ for Analyzing Compound-Target Engagement

Whether you’re looking to screen a library of drug candidates for binding to a particular target protein, checking drug cell…

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Blogs & Articles Do-It-Yourself: Benefits and Challenges of Creating Your Own Cell-Based Assays

Cell-based assays are useful for understanding cellular pathways; characterizing targets and their function; identifying, screening, and optimizing ligands or drugs…

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Blogs & Articles Critical Needs in Cellular Target Engagement

The development of new medicines for treating diseases and new chemical probes for elucidating biological function continues to rely on…

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Publications A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

A Potent, Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

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Publications Cell-Based Protein Stabilization Assays for the Detection of Interactions between Small-Molecule Inhibitors and BRD4

Bromodomain protein 4 (BRD4), a member of the bromodomain and extra-terminal (BET) proteinfamily, acts as a central element in transcriptional…

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Brochures & Flyers High-Throughput Screening & Lead Optimization Products

Robust Cell-Based Assays to Identify Therapeutic Hits Rapidly

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Brochures & Flyers Eurofins DiscoverX – Delivering Solutions from Discovery to Market

Products & Custom Development Capabilities.

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Target Lists Products Target List

Comprehensive Eurofins DiscoverX product list to enable your drug discovery and development programs focused on checkpoint receptors, cytokine receptors/interleukins, cytotoxicity,…

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Target Engagement Assays

Cell-based assays to confirm compound cell entry, protein target binding, screen & rank inhibitors, & measure cellular potencies

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Recombinant Proteins and Enzymes

Over 500 high-quality & purified recombinant kinases, phosphatases, & epigenetic & ubiquitin proteins

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Build Your Own Assay Tools

Complete set of parental cell lines, vectors, kits, & retroparticles to build your own stable cell lines & cell-based assays

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Custom Capabilities

Custom cell lines, kits, assays, & protein development capabilities optimized to fit your requirements

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