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Remarks
ML-385 is a potent and selective NRF2 inhibitor (Nrf2; IC50 = 1.9 µM) . ML-385 selectively intervenes therapeutic resistance in KEAP1-Deficient NSCLC Tumors. ML-385 inhibits its downstream target gene expression. ML385 binds to Neh1, the Cap 'N' Collar Basic Leucine Zipper (CNC-bZIP) domain of NRF2, and interferes with the binding of the V-Maf Avian Musculoaponeurotic Fibrosarcoma Oncogene Homologue G (MAFG)-NRF2 protein complex to regulatory DNA binding sequences. ML385 in combination with carboplatin showed significant antitumor activity.