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 activator-3 is a potent Nrf2 activator with potential anti-inflammatory, antioxidant, and anti-tumor activities, suitable for studying neurological and immune-related diseases.

Nrf2 degrader 30 is a small molecule PROTAC that inhibits the degradation of Nrf2, thereby enhancing its activity. Nrf2 is a key transcription factor that regulates cellular antioxidant responses and various protective mechanisms. The activity of Nrf2 is primarily regulated by its interaction with Keap1, which serves as an E3 ubiquitin ligase complex adapter to promote Nrf2 ubiquitination and proteasomal degradation。

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.

Nrf2 activator-12 (compound 10v) effectively activates Nrf2 (EC50=83.5 nM) and exhibits favorable pharmacological properties. It reverses disease progression and alleviates demyelination in a mouse model of experimental autoimmune encephalomyelitis.

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.

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 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.

Nrf2 activator-20 is a potent Nrf2 activator with anti-inflammatory and antioxidant properties. It activates anti-inflammatory pathways by disrupting the interaction between Keap1 and Nrf2, demonstrating beneficial effects in vivo. Nrf2 activator-20 is applicable for studies on acute respiratory distress syndrome (ARDS) and ischemia-reperfusion injury.

Nrf2 activator-21 is a compound that serves as an Nrf2 activator with both antioxidant and neuroprotective properties. It binds to the Keap1Kelch domain, disrupting the Keap1-Nrf2 interaction and activating antioxidant defense mechanisms. Nrf2 activator-21 decreases apoptosis of hippocampal neurons and reduces caspase-3 activity. It targets cerebral ischemia/reperfusion injury (CIRI) by activating the Nrf2 pathway. The compound improves neurological function, alleviates anxiety-like behavior induced by bilateral carotid artery occlusion (2VO) in rats, and enhances memory. Nrf2 activator-21 is applicable in studies of cerebral ischemia/reperfusion injury.

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/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-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].

Nrf2 activator-4 is an Nrf2 activator that inhibits the production of reactive oxygen species in microglia for the treatment of fatty liver disease associated with metabolic dysfunction in humans.

Nrf2 activator-5 is a potent activator of Nrf2 that attenuates H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglia, exhibiting antioxidant and anti-inflammatory activity.

AChE/Nrf2 modulator 1, an orally active compound, serves as a modulator of acetylcholinesterase (AChE) and nuclear factor erythroid 2-related factor 2 (Nrf2). It exhibits Nrf2 inductive activity alongside inhibitory effects on eeAChE and hAChE, demonstrating IC 50 values of 0.07 μM and 0.38 μM, respectively. This compound is applicable in Alzheimer's disease research.

Nrf2 Activator-6, a tetrahydroisoquinoline compound, functions as an Nrf2 activator, demonstrating potency with an IC50 value of 5 nM in inhibiting the Kelch domain-Nrf2 interaction.

Nrf2/HO-1-IN-1 is a potent Nrf2/HO-1 pathway inhibitor, with an IC 50 value of 0.38 μM for NO . Nrf2/HO-1-IN-1 can significantly reduce the level of ROS in cells. Nrf2/HO-1-IN-1 can be used for researching anti-inflammatory .

Nrf2 Activator-7 (Compound 12b) effectively enhances the Nrf2 signaling pathway as a potent Nrf2 activator.

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].

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].

Nrf2 degrader 1 (compound 1), a PROTAC Nrf2 degrader, exhibits anticancer properties by inhibiting the growth of cancer cells. It demonstrates IC 50 values of 100 nM for A549 cells and 40 nM for LK-2 cells, indicating potent efficacy [1].