nrf2 activator 1

Nrf2 activator-1 is a potent activator of NF-E2-related factor 2 (Nrf2) and can be used to study COPD and other respiratory diseases, including asthma, acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and pulmonary fibrosis.

Nrf2 activator 18 (Compound 11a) is an orally active activator of the Keap1 Nrf2 HO-1 signaling pathway, promoting Nrf2 nuclear translocation and enhancing antioxidant effects. It inhibits IL-6 release with an IC50 of 4.816 μM. In a mouse model of PM2.5-induced lung injury, Nrf2 activator 18 demonstrates anti-inflammatory activity.

Nrf2 HO-1 Activator 3 (Compound C3a) is an activator of the Nrf2 signaling pathway that facilitates the translocation of Nrf2 into the nucleus and enhances the expression of heme oxygenase-1 (HO-1). In H9c2 cardiomyocytes subjected to H2O2 or high glucose stimulation, Nrf2 HO-1 Activator 3 inhibits the excessive expression of ROS and MDA, suppressing cell viability and colony formation, thereby exhibiting antioxidant activity.

Nrf2 HO-1 activator 1 (Compound 24) is a potent neuroprotective and antioxidant agent targeting Nrf2 HO-1, with significant potential for therapeutic applications in Parkinson's disease (PD) research [1].

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 17 (compound 10) is an Nrf2 agonist that inhibits the interaction between Keap1 and Nrf2 with an IC50 value of <0.1 pM. In HepG2 cells, it demonstrates an EC50 of <10 μM.

VVD-130037 is a small molecule activator specifically targeting Kelch-like ECH-associated protein 1 (KEAP1) with potential antitumor activity.VVD-130037 inhibits tumor growth in advanced solid tumors by degrading NRF2.

Carnosol is an Nrf2 activator, increasing Nrf2 levels and promoting heme oxygenase 1 (HMOX1) expression. It is a ribosomal S6 kinase (RSK2) inhibitor and can be used in gastric cancer-related research with an IC50 value of approximately 5.5 μM.

CPDT is an orally active and potent inducer of phase 2 enzymes as well as an activator of Nrf2. CPDT enhances the activity of critical phase 2 enzymes, such as glutathione S-transferase, NAD(P)H:quinone oxidoreductase 1, and gamma-glutamylcysteine synthetase, and increases glutathione levels both in the bladder of rats and in bladder cells in vitro.

CBR-470-1 is a potent inhibitor of glycolytic phosphoglycerate kinase 1 (PGK1) that activates NRF2 by increasing methylglyoxal levels. CBR-470-1 is a non-covalent Nrf2 activator with neuroprotective activity that protects SH-SY5Y neuronal cells from MPP+-induced cytotoxicity by activating the Keap1-Nrf2 cascade. cytotoxicity induced by MPP+.

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 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].

Microcystin-LY, a cyclic heptapeptide toxin produced by the cyanobacterium Microcystis aeruginosa [2], is a potent activator of the Nrf2 pathway, inducing an oxidative stress response most effectively at a concentration of 3μM [1].

TAT-14 TFA is a 14-mer peptide functioning as an Nrf2 activator possessing anti-inflammatory properties. It does not alter Nrf2 mRNA expression but elevates Nrf2 protein levels by targeting the Nrf2 binding site on Keap1 [1].

Supercinnamaldehyde is a transient receptor potential anchor protein 1 (TRPA1) activator with thousands of anticancer and antimicrobial activities.Supercinnamaldehyde inhibits NF-κB signaling, induces cytoprotective responses and suppresses inflammatory responses through Nrf2 induction.Supercinnamaldehyde has been used in the study of bacterial infections.

Nrf2 Activator-8 (Compound 10e), with an EC50 of 37.9 nM, is a potent Nrf2 activator that demonstrates significant antioxidant and anti-inflammatory properties in BV-2 microglial cells. Furthermore, this compound notably ameliorates spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation [1].

S217879 is a potent and selective activator of NRF2 that disrupts the KEAP1-NRF2 interaction, resulting in significant activation of the NRF2 pathway. This compound is applicable in research on non-alcoholic steatohepatitis (NASH) [1].

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density lipoprotein (oxLDL) and high glucose (HG), also protecting vascular endothelial cells (VEC) from oxLDL and HG-induced injury, offering potential therapeutic benefits for atherosclerosis prevention and treatment [1].

R079 (compound 17), a selective and orally active Nrf2 activator, enhances Nrf2 translocation activity (EC 50 = 32.41 μM) and can neutralize excess levels of reactive oxygen species by activating Nrf2. Additionally, R079 possesses anti-inflammatory properties and has applications in multiple sclerosis research [1].

Fraxinellone analog 1 (compound 2) is an effective and rapid activator of the Nrf2-mediated antioxidative defense system, providing protection against glutamate-mediated excitotoxicity. It induces the expression of antioxidative genes Gpx4, Sod1, and Nqo1. Additionally, Fraxinellone analog 1 exerts neuroprotective effects and modulates oxidative stress and inflammation, making it suitable for research on neurodegenerative diseases.

(S)-(-)-Anatabine ((-)-Anatabine), an alkaloid present in tobacco, is an NRF2 activator that attenuates ovalbumin-induced asthma through oxidative stress and inflammation mitigation as well as up-regulation of Nrf2 HO-1 signaling in rats, and may be used in the study of autoimmune thyroiditis.

Nrf2 activator; inhibits Nrf2 Keap1 interaction. Induces upregulation of Nrf2 pathway downstream gene expression including heme-oxygenase 1. Suppresses LPS-induced TNF-α expression in THP-1 cells.