| S7672 |
Omaveloxolone (RTA-408)
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Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
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J Clin Invest, 2025, 135(14)e176655
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Redox Biol, 2025, 87:103885
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Front Pharmacol, 2025, 16:1539032
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| S8078 |
Bardoxolone Methyl (RTA 402)
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Bardoxolone Methyl (RTA 402, TP-155, NSC 713200, CDDO Methyl Ester, CDDO-Me) is an IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities; Also a potent Nrf2 activator and nuclear factor-κB (NF-κB) inhibitor. Bardoxolone Methyl abrogates ferroptosis. Bardoxolone methyl induces apoptosis and autophagy in cancer cells.
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J Clin Invest, 2025, 135(14)e176655
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Redox Biol, 2025, 87:103885
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Research (Wash D C), 2025, 8:0980
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| S8790 |
ML385
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ML385 is a novel and specific NRF2 inhibitor with an IC50 of 1.9 μM. It inhibits the downstream target gene expression of NRF2. This compound regulates the activity of several ferroptosis and lipid peroxidation-related proteins.
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Signal Transduct Target Ther, 2025, 10(1):323
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Redox Biol, 2025, 84:103657
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EMBO Mol Med, 2025, 10.1038/s44321-025-00293-5
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| S5771 |
Sulforaphane
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Sulforaphane is a naturally occurring isothiocyanate derived from the consumption of cruciferous vegetables, such as broccoli, cabbage, and kale. It is an inducer of Nrf2. This compound is also an inhibitor of histone deacetylase (HDAC) and NF-κB. It increases heme oxygenase-1 (HO-1) and reduces the levels of reactive oxygen species (ROS). It induces cell cycle arrest and apoptosis.
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J Clin Invest, 2025, 135(14)e176655
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Sci Rep, 2025, 15(1):21271
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BMC Cancer, 2025, 25(1):1050
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| S7956 |
Brusatol
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Brusatol (NSC 172924), isolated from the fruit of B. javanica, is a NRF2 inhibitor.
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EMBO Mol Med, 2025, 17(7):1794-1824
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J Zhejiang Univ Sci B, 2025, 26(9):881-896
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Neurochem Int, 2025, 188:106004
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| S4990 |
TBHQ
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Tert-butylhydroquinone (TBHQ) is an antioxidant compound which is used to prevent lipid peroxidation and shows multiple cytoprotective actions. It is an activator of Nrf2.
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Cancer Commun (Lond), 2025, 10.1002/cac2.70036
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Mol Med, 2025, 31(1):1
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J Zhejiang Univ Sci B, 2025, 26(9):881-896
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| S2586 |
DMF (Dimethyl Fumarate)
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Dimethyl Fumarate (DMF), the methyl ester of fumaric acid, is used to treat people with relapsing forms of multiple sclerosis. It is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
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J Clin Invest, 2025, 135(14)e176655
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Neural Regen Res, 2025, 10.4103/NRR.NRR-D-24-01469
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Chin Med, 2025, 20(1):61
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| S7864 |
Oltipraz
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Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
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Int Immunopharmacol, 2024, 143(Pt 1):113346
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J Neuroinflammation, 2023, 20(1):212
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PLoS Genet, 2022, 18(3):e1010128
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| S6647 |
Bardoxolone (CDDO)
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Bardoxolone (CDDO), acts by releasing Nrf2 from KEAP1,is a highly potent activator of Nrf2 that induce programmed cell death (apoptosis) in cancer cells.
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J Clin Invest, 2025, 135(14)e176655
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Sci Rep, 2025, 15(1):21271
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Int J Mol Sci, 2024, 25(15)8046
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| S5929 |
4-Octyl Itaconate
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4-Octyl Itaconate activates Nrf2 signaling to inhibit the production of pro-inflammatory cytokines in human macrophages and systemic lupus erythematosus (SLE) patient-derived PBMCs.
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Clin Transl Med, 2025, 15(7):e70419
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Biochem Biophys Res Commun, 2025, 747:151292
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Cell Death Dis, 2022, 13(6):521
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