Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene is a non-covalent inhibitor of the interaction between Kelch-like ECH-associated protein 1 (Keap1) and nuclear factor erythroid 2-related factor 2 (Nrf2). The Keap1–Nrf2 protein–protein interaction is considered a critical point of the Keap1–Nrf2–ARE (antioxidant response elements) system that protects cells from oxidative stress. Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene prevents Keap1 repression of Nrf2 activation, allowing Nrf2 to initiate antioxidant response element (ARE) to protect the cell. Bis-1,4-(4-methoxybenzenesulfonamidyl)naphthalene has an IC50 of 2.7 micromolar and specifically binds to the Keap1 Kelch-DC domain.
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