Nrf2

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.

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

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.

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.

Coniferaldehyde can significantly inhibit the growth of viability of strains of Oenococcus oeni. Coniferaldehyde exerts anti-inflammatory properties by inducing heme oxygenase-1(HO-1).

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.

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.

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.

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).

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.

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

Ezetimibe (SCH 58235) is a Dietary Cholesterol Absorption Inhibitor. The physiologic effect of ezetimibe is by means of Decreased Cholesterol Absorption.

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.

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.

Dimethyl fumarate (DMF), a fumarate derivative, is used as antiinflammatory and immunomodulatory agent.

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.

Mangiferin (Hedysarid) is used for antidiabetes. Extracted from Mangifera indica L.

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

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.

Danshensu (Dan shen suan A) is an active ingredient of Salvia miltiorrhiza with wide cardiovascular benefit.

AKOS B018304 is an aryl derivative capable of polarity substitution at the para position.AKOS B018304 is a chikungunya virus inhibitor.

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.

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

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.

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.

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.

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

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.

Ganodermanondiol exhibits potent cytoprotective effects on t-BHP-induced hepatotoxicity in human liver-derived HepG2 cells, presumably through Nrf2-mediated antioxidant enzymes and AMPK.

Latifolin is a strong DPPH-scavenger, it attenuates inflammatory responses by inhibiting NF-κB activation via Nrf2-mediated heme oxygenase-1 expression. Latifolin displays potent anticarcinogenic phase II marker enzyme, quinone reductase (QR) inducing activity and high chemopreventive indices. Latifolin also shows antifungal activity against white- and brown-rot fungi.

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

Dehydroglyasperin C is a potent NAD(P)H:oxidoquinone reductase (NQO1) and phase 2 enzyme inducer. Dehydroglyasperin C possesses potent antioxidant, cancer chemopreventive, and neuroprotective activities, it has protective effects against chronic diseases

Cudraflavone B has anti-proliferative activity, mouse brain monoamine oxidase (MAO) inhibitory effects, apoptotic actions in human gastric carcinoma cells and mouse melanoma cells, and hepatoprotective activity. It may be a lead for the development of a potential candidate for human oral squamous cell carcinoma cells.

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.

3',4',5',5,7-Pentamethoxyflavone is a naturally occurring brassinosteroid compound from the Rutaceae family that exhibits resistance to cancer cells by inhibiting the Nrf2 pathway to overcome chemotherapeutically active molecules.

Procyanidin B4 reveals significant antioxidant activity

Zederone has anti-bacterial activity,it inhibits gram-positive bacteria activity. Zederone induces hepatotoxicity implicated the induction of Cyps, which leads to the formation of biological reactive metabolites and that cause the oxidative stress and liver cell injuries.

6 -O-Malonyldaidzin (Daidzin 6''-O-malonate) may have anticancer activity.

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

Carlinoside could be a worthy choice to intervene hyperbilirubinemia due to liver dysfunction. Carlinoside upregulates Nrf2 gene expression, increases its nuclear translocation and stimulates UGT1A1 promoter activity.

NSC23925 is a selective and effective inhibitor of P-glycoprotein (Pgp).

Kinsenoside ((+)-Kinsenoside) shows significant antihepatotoxic, and anti-inflammatory activities. Kinsenoside could be useful for repairing beta cells in pancreatic islet injury as well as improving its function, it could promote the glucose tolerance of acute glucose increase in both diabetic and normal healthy rats. Kinsenoside inhibits osteoclastogenesis from macrophages by attenuating RANKL-induced NF-κB and NFATc1 activities, which in turn, prevents bone loss from OVX mice.

2-tert-Butyl-1,4-benzoquinone (TBQ), an electrophilic metabolite of butylated hydroxyanisole (BHA), causes activation of Nrf2 together with S-arylation of its negative regulator Keap1 in RAW264.7 cells.

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

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+.

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).

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

Pyridoxine (Vitamin B6) is the 4-methanol form of vitamin B6 and is converted to pyridoxal 5-phosphate in the body. Although pyridoxine and vitamin B6 are still frequently used as synonyms, especially by medical researchers, this practice is erroneous and sometimes misleading.

Ezetimibe, a compound known as a Niemann-Pick C1-like1 (NPC1L1) inhibitor and a potent Nrf2 activator, effectively inhibits cholesterol absorption. Additionally, Ezetimibe ketone (EZM-K) represents a phase-I metabolite of Ezetimibe.

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.