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Keap1-Nrf2 Nuclear factor (erythroid-derived 2)-like 2

Inhibitor/Activator

Cat.No.  Name Information
M8692 ML385 ML385 was a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM. ML385 inhibits Nrf2 transcription factor activity by binding to Neh1.
M10081 Omaveloxolone Omaveloxolone (RTA 408) is a first-in-class antioxidant inflammatory modulator (AIM) that activates Nrf2 and inhibits nitric oxide (NO). Omaveloxolone inhibits osteoclastogenesis by inhibiting the STING-dependent NF-κb signaling pathway.
M8710 Brusatol Brusatol (NSC 172924) is a plant-derived natural quassinoid that exhibits broad cytotoxicity in cancer cultures (IC50 <1 μM against 457 cancer cell lines) by inhibiting de novo synthesis of cellular proteins (Effective conc. <50 nM in A549 cells), including NRF2.
M40963 Tepilamide fumarate Tepilamide fumarate is an orally active Monomethyl fumarate (MMF) precursor compound that is also the Nrf2 stimulator, which can be used in studies related to psoriasis.
M39209 Toralactone Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
M39208 Artemisitene Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
M31251 CBR-470-1  CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
M30344 Carlinoside  Carlinoside is a flavone glycoside with hepatoprotective efficiency. Carlinoside reduces hepatic bilirubin accumulation by stimulating bilirubin-UGT activity through Nrf2 gene expression. Carlinoside has the potential to intervene hyperbilirubinemia due to liver dysfunction.
M30101 Hesperin  Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
M29865 Desfluoro-ezetimibe Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
M29455 DDO-7263  DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD).
M27939 Dibenzoylmethane Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
M27668 AEM1  AEM1 is a Nrf2 inhibitor. AEM1 reduces the expressions of Nrf2-dependent genes in A549 cells and inhibits the growth of A549 cells in vitro and in vivo.
M27629 Antroquinonol Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects. Antroquinonol can be used for the research of colon cancer. Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice.
M20776 cis-Resveratrol cis-Resveratrol (cis-RESV, cRes, (Z)-Resveratrol) is the Cis isomer of Resveratrol. Resveratrol is a natural phenolic compound with anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol is an inhibitor of pregnane X receptor (PXR) and an activator of Nrf2 and SIRT1 and may induce apoptosis.
M18767 L-Sulforaphane L-Sulforaphane is a highly potent inducer of the Keap1/Nrf2/ARE pathway.
M18155 Methyl 3,4-dihydroxybenzoate Methyl 3,4-dihydroxybenzoate




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