KEAP1-Nrf2 Inhibitor Screening Assay Kit

The Keap1:Nrf2 Inhibitor Screening Assay Kit is designed for identification of inhibitors of Keap1:Nrf2 binding using fluorescence polarization (FP), a powerful tool for studying molecular interactions by monitoring the change in rotational mobility of the fluorescently-labeled molecules upon their binding to a partner. To determine the effect of the inhibitor on the formation of Keap1:Nrf2 complexes the Keap1 protein and the fluorescent Nrf2 peptide are incubated with or without the test inhibitor for 30 minutes. Changes in rotational mobility of the Nrf2 peptide are measured using a plate readercapable of measuring fluorescence polarization.Figure 1. Illustration of the Keap1:Nrf2 Inhibitor Screening Assay Kit.This product has beencited 10 times.

Product Specifications

Background

Nuclear factor erythroid 2-related factor (Nrf2) is a transcription factor that coordinates antioxidant and anti-inflammatory responses by increasing the expression of antioxidant proteins through binding to theARE (antioxidant response element) region of their promoters. Under basal conditions, Nrf2 is retained in the cytosol by cytoskeletal Keap1, a substrate recognition subunit of a E3 ligase complex which targets Nrf2 for degradation. Exposure to oxidative stress causes the release of Nrf2 from Keap1. Nrf2 translocates to the nucleus, where it binds toAREsand induce the expression of antioxidant and phase II proteins protecting the cell from oxidative damage. Both Nrf2 and Keap1 are attractive therapeutic targets.

UniProt

Q14145

Applications

Great for studying enzyme kinetics and screening small molecule inhibitors for drug discovery and high-throughput applications.

Format

Catalog #NameAmountStorage70040Keap1, Human Recombinant*30 µg-80°CAvoid freeze/ thaw cycles79112FAM-Nrf2 peptide (10 µM) 10 µl-80°C79113Keap1-Nrf2 Assay Buffer10 ml-20°CBSA, 10 mg/ml100 µl-80°C7968596-well black plate1Room Temp*The concentration of the protein is lot-specific and will be indicated on the tube

Shipping Conditions

-80°C

Storage Conditions

This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.

Notes

Troubleshooting GuideVisitbpsbioscience.com/assay-kits-faqfor detailed troubleshooting instructions. For all further questions, please email[email protected]