Product News: TR-FRET readout now available with the Transcreener cGAMP cGAS Assay

With this addition, researchers can more easily screen for small molecule modulators of cGAS

26 Jan 2021


Launched in November 2019, the Transcreener cGAMP cGAS Assay has generated a great deal of interest in the drug discovery community. While fluorescence polarization (FP) readouts offer a stable and robust option, some researchers prefer time-resolved Förster-resonance-energy-transfer (TR-FRET) readouts for large screens. After months of development, BellBrook Labs is pleased to announce the addition of a TR-FRET readout to the Transcreener cGAMP cGAS Assay family.

Cyclic GMP-AMP synthase, or cGAS, is an enzyme recently identified as an innate immunity target. The cGAS-STING pathway has been shown to play a role in innate immune response, inflammation, tissue repair, infectious disease, and viral persistence. Investigating cGAS signaling events may lead to the discovery of small molecule modulators of this pathway for therapeutic intervention. High Throughput Screening is a powerful tool for cGAS discovery. In combination with Transcreener cGAMP cGAS Assay, researchers can use HTS to screen thousands of chemical compounds and discover active molecules, targeting the cause of inflammatory diseases. Upon detection of a positive hit in the HTS assay, the candidate compound can be advanced into functional and biochemical studies further to explore its potential as a novel therapeutic lead molecule.

BellBrooks customers provide a driving force to produce assays that enable quality data to accelerate their discovery efforts. Developing multiple fluorescent readouts allows researchers more tools for discovery. TR-FRET is one preferred option by many in drug discovery, especially in high throughput screening where time-gated measurements can help eliminate interference from the fluorescence of test compounds. The Transcreener cGAMP cGAS TR-FRET Assay is a simple mix-and-read format that provides excellent Z’ of greater than 0.7 at cGAMP ranges between 0.5 µM and 100 µM. It employs a far-red ATTO 647 tracer that further minimizes interference from fluorescent compounds and light scattering.

BellBrook Labs is a world leader in small molecule HTS research tools – our technology enables researchers to measure enzyme activity in a simple, high-throughput manner. Before the development of this assay, there were few options available for monitoring cGAS activity. Now, with Transcreener’s combination of two highly-sensitive fluorescent assays with robust high throughput capabilities, researchers can more easily screen for small molecule modulators of cGAS.

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