nrf2

Nrf2/HO-1 activator 2 (compound 13m), a difluoro-substituted derivative, is a highly potent activator of Nrf2/HO-1. It exhibits substantial neuroprotective and antioxidant properties by activating the Nrf2/HO-1 pathway through phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. This compound finds utility in the investigation of 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-3 is a potent Nrf2 activator with potential anti-inflammatory, antioxidant and anti-tumor activity, which can be used to study neurological and immune-related diseases.

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).

Keap1-Nrf2-IN-10 (compound 15) is a potent inducer of NQO1 and efficaciously mitigates oxidative stress in gamma-irradiated mice by reducing MDA and ROS levels, as well as NQO1 in the liver, which enhances the survival rate of these mice [1].

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].

Keap1-Nrf2-IN-9 (compound 11) is a potent inhibitor of the Keap1-Nrf2 protein−protein interaction (PPI) with an IC50 value of 0.575 µM. It enhances the expression of Nrf2 target genes, including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and glutamate-cysteine ligase catalytic (Gclc) and modulatory (Gclm) subunits. Notably, Keap1-Nrf2-IN-9 is not cytotoxic to ARPE19 cells [1].

Nrf2 activator-1 is a potent activator of NF-E2-related factor 2 (Nrf2).Nrf2 activator-1 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-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). It also protects vascular endothelial cells (VEC) from oxLDL and HG-induced injury, offering potential therapeutic benefits for the prevention and treatment of atherosclerosis [1].

Nrf2-Activator-12G is a potent Nrf-2 activator.

Nrf2-ARE/hMAO-B/QR2 modulator 1 is a new resveratrol-based multitarget-directed ligands (MTDLs) that showed a well-balanced MTDL profile: cellular activation of the NRF2-ARE pathway (CD = 9.83 μM), selective inhibition of both hMAO-B and QR2 (IC50s = 8.05 and 0.57 μM), and the best ability to promote hippocampal neurogenesis. Nrf2-ARE/hMAO-B/QR2 modulator 1 exerts neuroprotective and antioxidant actions in both acute and chronic Alzheimer models using hippocampal tissues.

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

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.

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 .

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.

Nrf2-IN-3 (Compound R16), a Nrf2 inhibitor, binds to KEAP1 mutants (G333C mKEAP1) thereby restoring the impaired KEAP1/NRF2 interactions. This restoration sensitizes KEAP1-mutant cancer cells to chemotherapeutic agents, such as Cisplatin and Gefitinib, by reestablishing the functionality of the mKEAP1/NRF2 complex [1].

Keap1-Nrf2-IN-15 (Compound 24a) is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, displaying IC50 values of 77 nM in a fluorescence polarization (FP) assay and 2.5 nM in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay [1].

Keap1-Nrf2-IN-16 is a biologically active peptide with KEAP1 binding activity.

Keap1–Nrf2 IN-1 activates Nrf2-regulated cytoprotective response and antagonizes acetaminophen-induced liver injury both in cellular and in vivo models. Keap1–Nrf2 IN-1 is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (

Keap1-Nrf2-IN-4, a powerful neddylation inhibitor, demonstrates significant anti-proliferation activity against MGC-803 cells (IC50 = 2.55 μM), effectively impeding their migration and inducing apoptosis. Additionally, it effectively inhibits tumor growth while exhibiting minimal toxicity [1].

Keap1-Nrf2-IN-1 TFA (compound35) is a Keap1-Nrf2 protein-protein interaction inhibitor (IC50: 43 nM) that activates Nrf2-regulated cytoprotective responses. Keap1-Nrf2-IN-1 TFA antagonizes acetaminophen-induced liver injury in cellular and in vivo models.

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).

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.

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

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-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-3 is a KEAP1:NRF2 protein protein interaction inhibitor, and with a K d value of 2.5 nM for KEAP1 protein.

Nrf2/HO-1 activator 1 (Compound 24) is a potent neuroprotective agent with significant antioxidant activities, specifically targeting Nrf2/HO-1. It is particularly useful in Parkinson's disease (PD) research, illustrating its potential in therapeutic applications [1].

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.

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.

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.

Omaveloxolone (RTA-408) (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.

ML385 is an NRF2 inhibitor (IC50=1.9 μM) with novelty and specificity. ML385 has anti-inflammatory activity by modulating anti-oxidative stress through the inhibition of NRF2. ML385 also exhibits anti-tumor activity.

4-Hydroxybenzyl alcohol (P-Methylolphenol) exhibits beneficial effects in cerebral ischemic injury, has neuroprotective effect through upregulation of Nrf2, Prdx6, and PDI expression via the PI3K/Akt pathway. 4-Hydroxybenzyl alcohol inhibit the development of new blood vessels by targeting multiple mechanisms of the angiogenic process, may as a promising candidate for the establishment of anti-angiogenic treatment strategies in cancer therapy.

L-Cystine dihydrochloride is an Nrf2 inducer with whitening and anti-dark spot effects.L-Cystine dihydrochloride has cytoprotective effects in cells, and is often added to various fungal cultures as a carbon source.

1. Farrerol has antioxidative activity.2. Farrerol modulates TAP and BNBD5 gene expression in mammary gland, enhances bMEC defense against S. aureus infection and could be useful in protection against bovine mastitis. 3. Farrerol inactivates KEAP-1 or act

1. Spinosin (Flavoayamenin) ameliorated memory impairment induced through AβO, the serotonergic neurotransmitter system, and these effects were regulated, in part, through neuroprotective activity via the anti-inflammatory effects of Spinosin. 2. Spinosin exerts anxiolytic-like effects, and its mechanism of action appears to be modulated by GABAA and 5-HT1A receptors. 3. There was a wide brain regional tissue distribution of Spinosin. The concentrations of Spinosin in corpus striatum and hippocampus were higher than that in other areas.

1. Oxyresveratro can inhibit tyrosinase activity. 2. Oxyresveratro is useful to trauma models, as toxicity to glia could be beneficial by inhibiting reactive gliosis. 3. Oxyresveratrol (trans-Oxyresveratrol) has antioxidant activity, can reduce neuronal oxidative damage and protect hepatocytes against oxidative stress and mitochondrial dysfunction, which may be associated with activation of Nrf2.

TAT 14 acetate, a 14-mer peptide, is an Nrf2 activator with anti-inflammatory properties. TAT 14 acetate increases Nrf2 protein levels due to targeting the Nrf2 binding site on Keap1, but has no effect on Nrf2 mRNA expression.

Cyclo(his-pro) is an endogenous cyclic dipeptide that exerts oxidative damage protection by selectively activating the transcription factor Nrf2 signalling pathway.

ethyl 2-[3,5-bis(trifluoromethyl)phenyl]-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxylate is a synthetic compound belonging to the curcumin family. It is involved in the regulation of immune response and inflammation through inhibition of the NF-κB signaling pathway, in the regulation of antioxidant response through activation of the Nrf2 signaling pathway, and in the regulation of cell survival and proliferation through inhibition of the Akt signaling pathway.

(E)-[6]-Dehydroparadol ((6)-Dehydroparadol), an oxidative metabolite of [6]-Shogaol, is a potent Nrf2 activator.

Antroquinonol is a ubiquinone derivative from Antrodia camphorata with anti-inflammatory and anticancer activities.Antroquinonol reduces oxidative stress and inhibits inflammation and sclerosis in mice with focal segmental glomerulosclerosis through enhancement of the Nrf2 signaling pathway.Antroquinonol has potential for use in the treatment of non-small cell lung cancer. Antroquinonol has potential for the treatment of non-small cell lung cancer and may be used in colon cancer research.

4-Octyl Itaconate is a cell-permeable derivative of Itaconate, an anti-inflammatory metabolite. 4-Octyl Itaconate activates Nrf2 via alkylation of KEAP1 and also inhibits phosphorylation of STING. 4-Octyl Itaconate is an anti-inflammatory metabolite.

Resveratrol (SRT 501) is a polyphenolic natural product, a plant antitoxin with antioxidant and chemopreventive activities. Resveratrol has a wide range of targets including COX, SIRT, LOC, etc. Resveratrol induces autophagy and apoptosis.

Fraxetin (7,8-dihydroxy-6-methoxy coumarin) has dual-antioxidative ,hepatoprotective and antihyperglycemic functions, it shows potent protective effects against CCl4 induced oxidative stress and hepatic fibrosis, has a marked inhibitory effect on S.aureus proliferation. It increased the level of Nrf2/ARE, and HO-1, inhibit the formation of ROS, cytochrome c release, activation of caspase-3 and 9, and suppressed the up-regulation of Bax.

ML162 is an inhibitor of GPX4 that is selectively lethal to mutant RAS oncogene-expressing cell lines (IC50s = 25 and 578 nM for HRASG12V-expressing and wild-type BJ fibroblasts, respectively)

4-hydroxyphenylacetic acid (parahydroxy phenylacetate) is a major microbiota-derived metabolite of polyphenols. 4-hydroxyphenylacetic acid(p-Hydroxyphenylacetic acid) is involved in the antioxidative action. 4-hydroxyphenylacetic acid(p-Hydroxyphenylacetic acid) induces expression of Nrf2.