nrf2/are

Keap1/Nrf2/ARE activator 1 (compound HT-3) functions as an activator of the Keap1/Nrf2/ARE pathway. This compound has antioxidant properties and offers neuroprotective effects.

Nrf2-ARE/hMAO-B/QR2 modulator 1, a resveratrol derivative and multi-target-directed ligand (mtdl), activated the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibited hMAO-B and QR2（quinone reductase-2，NQO2) (IC 50 = 8.05 and 0.57 μM), and was able to promote hippocampal neurogenesis and exert neuroprotective and antioxidant effects in an Alzheimer's disease model.

CDDO-EA (CDDO ethyl amide) is an activator of the Nrf2/antioxidant response element.

1. Isoquercetin (3-Glucosylquercetin) is a potential stimulator of bone mineralization used for prophylaxis of osteoporotic disorders. 2. Isoquercetin may be as a potential therapeutic agent against neurodegeneration in Parkinson's disease. 3. Isoquercetin is an inhibitor of Wnt/β-catenin and may be as a potential novel anti-tumoral agent, such as against human pancreati,liver cancer related to opioid receptors and to the activation of the mitogen-activated protein kinase (MAPK) signalling pathway. .

Sesaminol is an orally active activator of the Nrf2-ARE signaling pathway, promoting the nuclear translocation of Nrf2 and boosting the expression of NQO1 to enhance cellular defense against oxidative stress. It inhibits 6-OHDA-induced ROS production and apoptosis in SH-SY5Y cells. Sesaminol also provides neuroprotective effects against Rotenone-induced Parkinson's disease.

KEAP1-NRF2PPI-IN-1 (compound 23) is an inhibitor targeting the KEAP1-NRF2 interaction. In DNA damage tests, its IC50 values are 136 nM in human TK6 cell lines and 62 nM in insect SF9 cell lines.

Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a strong activity showing an ED50 of 0.04 mmol/kg. By inhibiting the Keap1-Nrf2 binding, it activates the Nrf2/ARE pathway, providing anticonvulsant and neuroprotective effects, making it useful for research in epilepsy and neuroprotection.

Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent antioxidant response element (ARE) inducer, with an EC50 of 2.7 μM, and also acts as an Nrf2 activator. It modifies Keap1, preventing the formation of the Cul3-Keap1 ubiquitin ligase complex, thereby activating Nrf2 transcription. Nrf2 activator-10 provides cellular protection against H2O2-induced apoptosis.

Keap1-IN-2 (Compound 164) is an inhibitor of KEAP1 with an IC50 of 2 nM. It indirectly activates Nrf2 by blocking KEAP1, thereby enhancing cellular antioxidant capacity. By preventing KEAP1-mediated degradation of Nrf2, Keap1-IN-2 promotes the accumulation and nuclear translocation of Nrf2. This compound is used in research on diseases related to oxidative stress, such as inflammatory bowel disease, Crohn's disease, and ulcerative colitis, which are immune-related conditions.

Pyrraline is an activator of the Nrf2 pathway with antioxidant and anti-inflammatory properties. It enhances antioxidant enzymes like NAD(P)H oxidase (NQO1) and heme oxygenase-1 (HO-1) by activating the antioxidant response element (ARE), while inhibiting inflammation mediated by NFκB. Pyrraline holds potential for research in metabolic disorders, such as diabetic nephropathy, and cancer.

CPUY192018 is an inhibitor of Keap1-Nrf2 protein-protein interactions and shows cytoprotective effects in NCM460 colon cells.CPUY192018 inhibits glycolysis, enhances resistance to oxidative stress, and can be used to study mitochondrial autophagy.

Fraxetin (7,8-dihydroxy-6-methoxy coumarin) has dual-antioxidative ,hepatoprotective and antihyperglycemic functions, it shows potent protective effects against CCl4 induced oxidative stress and hepatic fibrosis, has a marked inhibitory effect on S.aureus proliferation. It increased the level of Nrf2/ARE, and HO-1, inhibit the formation of ROS, cytochrome c release, activation of caspase-3 and 9, and suppressed the up-regulation of Bax.

Gypenoside XVII (Gynosaponin S) confers protection against Aβ25-35-induced neurotoxicity through estrogen receptor-dependent activation of PI3K/Akt pathways, activation of Nrf2/ARE/HO-1 and inactivation of GSK-3β pathways.

1. 5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) isolated from DME is one of the active compounds that may contribute to regulate blood glucose levels. 2. 5,7-Dihydroxychromone exerts neuroprotective effect against 6-OHDA-induced oxidative stress and apoptosis by activating Nrf2/ARE signal . 3. 5,7-Dihydroxychromone induces the translocation of Nrf2 to the nucleus and increases Nrf2/ARE binding activity which results in the up-regulation of the expression of Nrf2-dependent antioxidant genes, including HO-1, NQO1, and GCLc.

DDO-7263 is a 1,2,4-Oxadiazole derivative that upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 is a potent Nrf2 activator that activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity [1].

Shinorine, a mycosporine-like amino acid (MAA), is a small molecule sunscreen produced in some bacteria. Shinorine ameliorates chromium induced toxicity in zebrafish hepatocytes through the facultative activation of Nrf2-Keap1-ARE pathway. Shinorine is also an analogue of porphyra-344. Both porphyra-334 and shinorine are antioxidants and direct antagonists of Keap1-Nrf2 binding. Shinorine may be a useful agent to prevent or retard the progression of multiple degenerative disorders of ageing. Shinorine is a demethyl-analog of Porphyra 334.

2-HBA, a synthetic analog of curcumin, is an indirect inducer of enzymes that catalyze detoxification reactions through the Keap1-Nrf2-ARE pathway.

(R)-Sulforaphane (L-Sulforaphane) is a potent inducer of the Keap1/Nrf2/ARE pathway.

HPO-DAEE (4-Hydroperoxy-2-decenoic acid ethyl ester) performs multiple roles in cellular processes, primarily enhancing nuclear accumulation of Nrf2 and activating the antioxidant response element (ARE). It upregulates antioxidant genes such as HO-1 through Nrf2-ARE signaling and initiates the generation of reactive oxygen species. Additionally, HPO-DAEE inhibits histone deacetylase, promoting the expression of extracellular superoxide dismutase via histone acetylation. It offers protection against 6-hydroxydopamine-induced cell death by activating the Nrf2-ARE and eIF2α-ATF4 pathways [1].

5,7-Dihydroxychromone (Standard) is a reference standard for research and analysis in studies involving 5,7-Dihydroxychromone. 1. 5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) isolated from DME is one of the active compounds that may contribute to regulate blood glucose levels. 2. 5,7-Dihydroxychromone exerts neuroprotective effect against 6-OHDA-induced oxidative stress and apoptosis by activating Nrf2/ARE signal . 3. 5,7-Dihydroxychromone induces the translocation of Nrf2 to the nucleus and increases Nrf2/ARE binding activity which results in the up-regulation of the expression of Nrf2-dependent antioxidant genes, including HO-1, NQO1, and GCLc.

Gypenoside XVII (Standard) is a reference standard for research and analysis in studies involving Gypenoside XVII. Gypenoside XVII (Gynosaponin S) confers protection against Aβ25-35-induced neurotoxicity through estrogen receptor-dependent activation of PI3K/Akt pathways, activation of Nrf2/ARE/HO-1 and inactivation of GSK-3β pathways.

Fraxetin (Standard) is a reference standard for research and analysis in studies involving Fraxetin. Fraxetin (7,8-dihydroxy-6-methoxy coumarin) has dual-antioxidative ,hepatoprotective and antihyperglycemic functions, it shows potent protective effects against CCl4 induced oxidative stress and hepatic fibrosis, has a marked inhibitory effect on S.aureus proliferation. It increased the level of Nrf2/ARE, and HO-1, inhibit the formation of ROS, cytochrome c release, activation of caspase-3 and 9, and suppressed the up-regulation of Bax.

Isoquercetin (Standard) is a reference standard for research and analysis in studies involving Isoquercetin. 1. Isoquercetin (3-Glucosylquercetin) is a potential stimulator of bone mineralization used for prophylaxis of osteoporotic disorders. 2. Isoquercetin may be as a potential therapeutic agent against neurodegeneration in Parkinson's disease. 3. Isoquercetin is an inhibitor of Wnt/β-catenin and may be as a potential novel anti-tumoral agent, such as against human pancreati,liver cancer related to opioid receptors and to the activation of the mitogen-activated protein kinase (MAPK) signalling pathway. .

Azafrin is a carotenoid and one of the most abundant active components in C. grandiflora. It enhances the expression of HO-1, NQO1, and Nrf2 and protects the myocardium by activating the Nrf2-ARE pathway, countering myocardial damage. Azafrin is applicable in cardiovascular disease research.