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/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.

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/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].

Keap1/Nrf2/ARE activator 2 is an activator of the Keap1/Nrf2/ARE pathway, acting as a non-competitive inhibitor of AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. It enhances Nrf2 nuclear translocation, thereby upregulating antioxidant gene expression and boosting cellular defenses against oxidative stress. In PC12 cells, Keap1/Nrf2/ARE activator 2 demonstrates significant neuroprotective effects against damage induced by H2O2 and Scopolamine (SCA). In zebrafish models, it alleviates cognitive deficits and neuroinflammation associated with SCA-induced impairments. This compound is relevant for Alzheimer's disease research.

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 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 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-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-12G (compd 12g) is a direct activator of Nrf2 that induces robust expression of Nrf2-dependent antioxidant enzymes at both mRNA and protein levels in dopaminergic neuronal cells, thereby enhancing cellular defense against oxidative stress and providing a mechanistic platform for investigating neuroprotection and disease-modifying strategies in Parkinson’s disease research.

Nrf2 activator-11 (compound M11) is a Nrf2 activator that possesses blood-brain barrier permeability and offers anti-oxidation, anti-inflammation, anti-ferroptosis, and anti-apoptosis properties. It is applicable for use in studying cerebral ischemia-reperfusion (CI/R) injury models.

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.

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.

KMS99220 is an orally active Keap-1 activator that acts as an Nrf2 inhibitor protein. It enhances Nrf2 nuclear translocation, increases the expression of antioxidant enzymes (such as heme oxygenase-1) and proteasome subunit genes, and alleviates oxidative stress and protein aggregation damage. KMS99220 is applicable for research in Parkinson's disease (PD).

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.

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].

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.

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].