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An inhibitor of the Nrf2-Keap1 protein-protein interaction
ML-334 is an inhibitor of the protein-protein interaction between the transcription factor Nrf2 and its inhibitor Keap1.1 It binds to the Keap1 Kelch domain (IC50 = 1 ?M) to induce dissociation and nuclear translocation of Nrf2 and activation of the antioxidant response element (ARE) in a cell-based assay (EC50 = 12 ?M).
1.Hu, L., Magesh, S., Chen, L., et al.Discovery of a small-molecule inhibitor and cellular probe of Keap1-Nrf2 protein-protein interactionBioorg. Med. Chem. Lett.23(10)3039-3043(2013)
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