| Description: | 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 re |
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| Background: | 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. |
| UniProt | Q14145 |
| Synonym(s): | Kelch-like ECH-associated protein, INRF2, KIAA0132, KLHL19 |
| Supplied As: | The kit comes in a convenient 96-well format, with purified Keap1 protein, a fluorescently labeled Nrf2 peptide containing the ETGE motif, and assay buffer for 100 protein reactions |
| Format: | |
| Instructions for use: | See assay kit data sheet for detailed protocol. |
| Storage / Stability: | At least 6 months from date of receipt when stored as directed. |
| Application(s): | Great for screening small molecular inhibitors for drug discovery and HTS applications. |
| Reference(s): | Inoyama, D., et al. 2012. J. Biomol. Screening 17(4): 435-447. |
| Notes: | MATERIALS REQUIRED BUT NOT SUPPLIED: Plate reader capable of fluorescence polarization measurements, ex = 475-495 nm, em = 518-538 nm. Adjustable micropipettor and sterile tips |
| Warning(s): | Avoid freeze/thaw cycles. Protect Nrf2-FITC from light. |
| Scientific Category: | Other Proteins |
| Product Type: | Assay Kits |