Autotaxin (ATX) Inhibitor Screening Service
The Autotaxin (ATX) Inhibitor Screening Service utilizes the ATX Inhibitor Screening kits (cat #’s K-4200 or K-4200HTS) to determine if your compound inhibits ATX. ATX is an extracellular enzyme that cleaves lysophosphatidylcholine (LPC) to generate the phospholipid growth factor lysophophatidic acid (LPA). LPA is involved in a variety of biological functions, such as angiogenesis, wound healing, vascular and nervous system development, reproduction, pain transmission, immunological competence and the regulation of blood pressure. Altered LPA biology is associated with a number of diseases. Likewise, autotaxin has been implicated in a number of disorders, including a variety of cancers, obesity, arthritis, multiple sclerosis, Alzheimer’s disease and neuropathic pain.
- Echelon has 25 years of assay development expertise and 15 years experience in the ATX field.
- Your compounds are cataloged and stored according to your requirements.
- The ATX inhibitor Screening Service will run each compound in duplicate, in two screens.
- Results are provided as % inhibition or IC50, if a full inhibitor curve is ran.
- Usually, results are provided 2 weeks from receipt of samples. We can accommodate tighter schedules if needed.
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ATX inhibition is determined in the ATX inhibitor screening kit (cat #’s K-4200 or K-4200HTS). These assays utilize the fluorogenic substrate, FS-3, an LPC analogue, that is conjugated with both a fluorophore and a quencher. When ATX cleaves FS-3, the fluorophore becomes liberated from the quencher, resulting in increased fluorescence.
In this assay service, two screens are ran for each compound. In the initial screen, recombinant ATX is incubated with your inhibitor(s) or a control inhibitor (BrP-LPA). The substrate, FS-3, is then added subsequently and fluorescence is measured over time. These assays are continuous (not end point) and have the advantage of being less susceptible to error arising from mistiming in the addition of reagents.
The secondary screen is performed to evaluate whether a sample hit, revealed in the initial screen, is a false positive due to interference with the assay. The sample inhibitors that are positive in the initial screen and negative in the secondary screen are potential ATX inhibitors.
Test results will be provided as % inhibition or IC50. All data points will be run in duplicate and reported as an average.
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