nrf 2

Nrf2-IN-1 is an nuclear factor-erythroid 2-related factor 2 (Nrf2) inhibitor. Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).

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-12G is a potent Nrf-2 activator.

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.

Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of the protein-protein interaction between Keap1 and Nrf2.

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-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-IN-4 is an Nrf2 inhibitor that induces ferroptosis by disrupting cellular iron homeostasis, promoting ferritin degradation, and ultimately triggering ferroptosis. It activates lysosomes through iron-dependent reactive oxygen species (ROS) production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor effects and is applicable in breast cancer research.

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-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.

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.

Keap1-Nrf2-IN-5 is a potent inhibitor of Keap1-Nrf2 PPI (Keap1-Nrf2 protein-protein interaction) (IC50: 4.1 μM, Kd: 3.7 μM).

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.

Keap1-Nrf2-IN-14 is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50: 75 nM) with a Kd=24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and is able to enhance downstream antioxidant and anti-inflammatory effects. -Nrf2-IN-14 can be used to study oxidative stress-related inflammation.

eap1-Nrf2-IN-12 is a potent inhibitor of Keap1-Nrf2 (IC50: 2.30 μM). eap1-Nrf2-IN-12 is metabolically stable in human liver microsomes.

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.

Keap1-Nrf2-IN-11 (Compound 6k), a potent Keap1-Nrf2 inhibitor, exhibits a dissociation constant (KD) of 0.21 nM. It hampers the production of reactive oxygen species (ROS) and nitric oxide (NO), as well as the expression of tumor necrosis factor-alpha (TNF-α). By promoting Nrf2 nuclear translocation, it mitigates inflammation and is utilized in anti-inflammatory studies [1].

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.

Keap1-Nrf2-IN-13 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI) with an IC50 value of 0.15 μM, indicating high efficacy. It binds strongly to Keap1 by forming hydrogen bonds with critical polar residues (Asn414, Arg415, Arg483, Gln530), showcasing specificity. This compound has implications for research into diseases associated with oxidative stress and inflammation, such as pulmonary fibrosis, chronic obstructive pulmonary disease (COPD), and cancers, due to its mechanism of action.

Keap1-Nrf2-IN-6 is a potent, selective inhibitor of the Keap1-Nrf2 protein−protein interaction (PPI), demonstrating an inhibitory concentration (IC50) of 41 nM and a dissociation constant (Kd) of 68 nM.