Nrf2

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.

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

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

Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

Sulforaphane is a natural isothiocyanate that activates Nrf2 and inhibits AMPK-dependent signaling. Sulforaphane has antitumor and anti-inflammatory activities by increasing the transcription of tumor suppressor proteins and inhibiting histone deacetylase activity.

Brusatol (NSC-172924) is a natural product isolated from the Brucea javanica plant. It inhibits Nrf2.

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.

KI696 is a high-affinity probe that potently inhibits the interaction of Keap1 and NRF2.

1. Eriodictyol (Huazhongilexone) is a flavonoid with anti-inflammatory and antioxidant activities. 2. Eriodictyol may possess antidiabetic properties through increasing glucose uptake and improving insulin resistance. 3. Eriodictyol may be a potential therapeutic resource for Atopic dermatitis and an adjunctive agent to control itchiness inAtopic dermatitis.

CDDO-EA (CDDO ethyl amide) is an activator of the Nrf2/antioxidant response element.

Tricetin is a flavonoid isolated from pomegranate.Tricetin is a potent competitive inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) and protects Parkinson's disease patients from 6-OHDA-induced neurotoxicity by activating the Nrf2 HO-1 signaling pathway and blocking mitochondria-dependent apoptotic pathways.Tricetin Inhibits migration and expression of the indicator protease progerin-1 (PS-1) in nasopharyngeal carcinoma through the Akt GSK-1β pathway.Tricetin inhibits endothelial inflammation induced by oxidized LDL mediated by Egr-1, and protects rat chondrocytes from IL-1β-induced inflammation and apoptosis.Tricetin is an inhibitor of endothelial inflammation induced by oxidized LDL mediated by Egr-1 and protects against IL-1β-induced inflammation and apoptosis.

Ezetimibe (SCH 58235) is a dietary cholesterol absorption inhibitor that exerts its physiologic effect by decreasing cholesterol absorption.

Sappanone A is a high isoflavanone that exhibits anti-inflammatory effects by modulating Nrf2.Sappanone A attenuates allergic airway inflammation in ovalbumin-induced asthma.

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.

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.

Rosolutamide (ALZ-003) is a curcumin analog, an orally active Nrf1 and Nrf2 activator.Rosolutamide modulates oxidative homeostasis, improves mitochondrial function and promotes autophagy, reduces mutant protein aggregation, and decreases intracellular mitochondrial reactive oxygen species (ROS) levels.Rosolutamide has been used in the study of neurodegeneration such as spinal cerebellar ataxia and Huntington disease. neurodegenerative diseases such as Huntington's disease. Regulates oxidative homeostasis.

Danshensu (Dan shen suan A) is an active ingredient of *Salvia miltiorrhiza* with extensive cardiovascular benefits.

CDDO-Im (TP-235) is an activator of Nrf2 and PPAR (Kis: 232 344 nM for PPARα PPARγ).

Hydrangenol is a natural product and can be isolated from Hydrangea serrata leaves. Hydrangenol is an antiphotoaging compound with oral activity. Hydrangenol can reduce MMP and inflammatory cytokine expression and increase moisturizing factors and antioxidant genes level, result in preventing wrinkle formation.

Bardoxolone (CDDO) is a synthetic oleanane triterpenoid that blocks the cellular synthesis of inducible nitric oxide synthase and inducible COX-2 in INF-γ-activated mouse macrophages with an IC50 value of 0.4 nM. By suppressing reactive oxygen and nitrogen species (ROS RNS) formation, it promotes the cellular control of ROS RNS levels that would lead to DNA damage associated with tumorigenesis. In various Y cell lines, Bardoxolone has been shown to specifically inhibit proliferation and induce apoptosis. Mechanism studies revealed that Bardoxolone is a ligand for peroxisome proliferator-activated receptor γ, and also that it induces genes regulated by Nrf2, including heme oxygenase-1 and eotaxin-1, which play a role in antioxidant response element signaling activity.

Bardoxolone Methyl (TP-155) is a synthetic triterpenoid that acts as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway with potential anti-tumor and anti-inflammatory activities.

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.

TBHQ (tert-Butylhydroquinone) is an antioxidant that induces an antioxidant response through the redox-sensitive transcription factor Nrf2.

1. Corynoline ((+)-Corynoline) is an acetylcholinesterase inhibitor.

Eriodictyol-7-O-glucoside is an Nrf2 activator conferring protection against Cisplatin-induced toxicity. Eriodictyol-7-O-glucoside is a flavonoid and a free radical scavenger with antioxidant activity in pistachio skin.

CDDO-dhTFEA, a synthetic oleanane triterpenoid, effectively activates Nrf2 while inhibiting the NF-κB pro-inflammatory transcription factor. It restores mean arterial pressure (MAP), elevates Nrf2 levels and the expression of related genes, attenuates NF-κB and transforming growth factor-β pathway activation, and mitigates glomerulosclerosis, interstitial fibrosis, and inflammation in rats with chronic kidney disease (CKD).

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).

Astilbin (Neoastilbin) is actions Flavonoid phytochemical found in St. John′s wort and Traditional Chinese Medicine herbal preparations.

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

Physalin B is one of the major active compounds from the Solanaceae family of plants and has a wide range of biological activities for the treatment of inflammatory eczema and herpes, among other diseases.Physalin B ameliorates lipopolysaccharide-induced inflammatory response due to acute lung injury by inhibiting NF-κB and NLRP3 through activation of the PI3K Akt pathway.Physalin B inhibits PDGF-BB-induced VSMC proliferation and migration and phenotypic transformation through activation of the Nrf2 pathway. Physalin B inhibits PDGF-BB-induced VSMC proliferation, migration and phenotypic transformation through activation of the Nrf2 pathway.Physalin B exerts antitumor activity by inhibiting LAP2α-HDAC1-mediated deacetylation of glioma-associated oncogene 1 and hepatic stellate cell activation.

Pelargonidin chloride shows protective effect against CTN-induced oxidative stress in HepG2 cells and up-regulated the activity of detoxification enzyme levels through Keap1 Nrf2 signaling pathway.

Nrf2-IN-3 is a mKEAP1-selective NRF2 inhibitor that selectively binds KEAP1 mutants and restores their NRF2 inhibitory function by repairing the disrupted KEAP1 NRF2 interaction, and selectively sensitizes cisplatin in xenografts of mouse mKEAP1 cancer cells.

AEM1 is an inhibitor of deregulated NRF2 transcriptional activity in cancer. AEM1 acts by broadly decreasing the expression of NRF2 controlled genes, sensitizing A549 cells to various chemotherapeutic agents, and inhibiting the growth of A549 cells in vitro and in vivo.

Notoginsenoside R2 (20(S)-Notoginsenoside R2) has neuroprotection against 6-OHDA-induced neurotoxicity, is associated with Notoginsenoside R2-mediated P90RSK and Nrf2 activation through MEK1 2-ERK1 2 pathways.

NK-252 is a potential activator of Nrf2. It has great Nrf2-activating potential.

(-)-Butin (Butin) has antioxidant activity, can protect cells against H2O2-induced apoptosis, oxidative DNA damage and oxidative mitochondrial dysfunction; it attenuates oxidative stress by activating Nrf2-mediated Mn SOD induction via the PI3K Akt signaling pathway.

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+.

(R)-Sulforaphane (L-Sulforaphane) is a potent inducer of the Keap1 Nrf2 ARE pathway.

Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester), a key metabolite of antioxidant polyphenols in green tea, exhibits significant antioxidant and anti-inflammatory properties.

Tigloylgomisin H represents a potential liver cancer prevention agent, it can significantly induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells, it functions as a novel monofunctional inducer that specifically upregulates phase

I-152 is a coupling of N-acetylcysteine and β-mercaptoethylamine. I-152 has antiproliferative, antiviral, and immunomodulatory activities. I-152 is used in the study of viral infections because it activates NRF2 and ATF4 signaling.

K67 competitively inhibits the interaction between Nrf2-ETGE and Keap1, inhibits the proliferation of HCC cells with high expression of S351 phosphorylated p62, and can be used to study cancer.

1. 5,7-Dihydroxychromone (5,7-Dihydroxy-4H-Chromen-4-One) isolated from DME is one of the active compounds that may contribute to regulate blood glucose levels. 2. 5,7-Dihydroxychromone exerts neuroprotective effect against 6-OHDA-induced oxidative stress and apoptosis by activating Nrf2 ARE signal . 3. 5,7-Dihydroxychromone induces the translocation of Nrf2 to the nucleus and increases Nrf2 ARE binding activity which results in the up-regulation of the expression of Nrf2-dependent antioxidant genes, including HO-1, NQO1, and GCLc.

4-Acetoxyphenol Prevents RPE Oxidative Stress-Induced Necrosis by Functioning as an NRF2 Stabilizer

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].

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.

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

2-tert-Butyl-1,4-benzoquinone (TBQ), an electrophilic metabolite of butylated hydroxyanisole (BHA), activates Nrf2 and S-arylates its negative regulator Keap1 in RAW264.7 cells.