||The nuclear factor erythroid 2-related factor (Nrf2) is a transcription factor that induces the expression of antioxidant and phase II proteins by binding to the ARE (antioxidant response element) region of the gene promoter. Under basal conditions, Nrf2 is retained in the cytosol by binding to the cytoskeletal protein Keap1. Upon exposure to oxidative stress and other ARE activators, Nrf2 is released from Keap1. It then translocates to the nucleus, where it can bind to the ARE and activate expression of antioxidant and phase II proteins that protect the cell from oxidative damage. Because Nrf2 activation leads to a coordinated antioxidant and antiinflammatory response, and Keap1 represses Nrf2 activation, Keap1 has become a very attractive drug target.
||The Keap1:Nrf2 Inhibitor Screening Assay Kit is designed for identification of inhibitors of Keap1:Nrf2 binding using fluorescence polarization. Using this kit, only one simple step on a microtiter plate is required for Keap1:Nrf2 inhibitor screening reactions. The Keap1 protein and fluorescently labeled Nrf2 peptide are incubated with a sample containing testing inhibitors for 30 minutes. The change in fluorescent polarization can then be measured using a fluorescence reader.
||Great for screening small molecular inhibitors for drug discovery and HTS applications.
||At least 6 months from date of receipt when stored as directed.
||Keap1, human recombinant: 30 µg; -80°C Nrf2 peptide, FITClabeled (10 µM): 10 µl; -80°C Keap1-Nrf2 Assay Buffer: 50 ml; -20°C BSA, 10 mg/ml: 100 µl; -80°C 96-well plate: 1; +4°CAvoid freeze/thaw cycles. Protect Nrf2-FITC from light.