nrf2/are pathway

Wnt pathway activator 2, with an IC50 of 13 nM, is a potent Wnt activator.

Nrf2 HO-1 activator 2 (compound 13m), a difluoro-substituted derivative, is a highly potent activator of Nrf2 HO-1 with substantial neuroprotective and antioxidant properties. It functions by activating the Nrf2 HO-1 pathway through the phosphorylation of ERK1 2, JNK, or Akt in PC12 cells and is useful in investigating Parkinson's disease (PD) [1].

Nrf2 activator-2 (referred to as compound O15), an Osthole derivative, is a highly potent Nrf2 agonist exhibiting an EC 50 of 2.9 μM in 293 T cells. By effectively disrupting the binding between Keap1 and Nrf2, Nrf2 activator-2 activates the Nrf2 pathway. Furthermore, this compound significantly reduces the ubiquitination of Nrf2 in cells, indicating its potential in regulating Nrf2 activity [1].

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. .

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

Tigloylgomisin H represents a potential liver cancer prevention agent, it can significantly induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells, it functions as a novel monofunctional inducer that specifically upregulates phase

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

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].

Nrf2-ARE hMAO-B QR2 modulator 1, a new resveratrol-based multitarget-directed ligand (MTDL), exhibits a well-balanced MTDL profile: it activates the NRF2-ARE pathway (CD = 9.83 μM), selectively inhibits both hMAO-B and QR2 (IC50s = 8.05 and 0.57 μM), and effectively promotes hippocampal neurogenesis. It exerts neuroprotective and antioxidant actions in both acute and chronic Alzheimer models using hippocampal tissues.

(R)-5-Hydroxy-1,7-diphenylheptan-3-one ((5R)-Dihydroyashabushiketol) is extracted from the rhizomes of Alpinia officinarum, a Chinese medicinal herb, and inhibits melanogenesis in theophylline-stimulated murine B16 melanoma 4A5 cells.

Rehmapicrogenin regulates the Nrf2 ARE signaling pathway. Nrf2 ARE signaling pathway is the most important pathway of oxidative stress.

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.