2. Signaling Pathways
  3. NF-κB
  4. Keap1-Nrf2

Keap1-Nrf2

Keap1-Nrf2

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Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS). Keap1 is an E3 ligase, which induces the degradation of Nrf2 by ubiquitin-proteasome system (UPS). Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. For this case, Nrf2 is an attractive molecule as a therapeutic target in cancer and a lot number of Nrf2 inhibitors are developed. What’s interesting, Nrf2 induction is also reported to be treatment strategies for accelerating the detoxification of carcinogens and protect the body from chemical carcinogenesis.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-19893
    Antroquinonol
    		Activator 98.61%
    Antroquinonol ((+)-Antroquinonol), a ubiquinone derivative from the mushroom Antrodia camphorata, has hepatoprotective, anti-inflammatory, and anti-cancer effects. Antroquinonol can be used for the research of colon cancer. Antroquinonol reduces oxidative stress by enhancing the Nrf2 signaling pathway and inhibits inflammation and sclerosis in focal segmental glomerulosclerosis mice.
    Antroquinonol
  • HY-159495
    Keap1-Nrf2-IN-21
    Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the Keap1-Nrf2 signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC50=2.60 μM).
    Keap1-Nrf2-IN-21
  • HY-W009731R
    Dibenzoylmethane (Standard)
    		Activator
    Dibenzoylmethane (Standard) is the analytical standard of Dibenzoylmethane. This product is intended for research and analytical applications. Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
    Dibenzoylmethane (Standard)
  • HY-168526
    Keap1-Nrf2-IN-24
    		Inhibitor
    Keap1-Nrf2-IN-24 (compound 57) is a potent Keap1-Nrf2 inhibitor with a Ki value of 13 nM. Keap1-Nrf2-IN-24 increases the protein expression of TRXR1 and NQO1. Keap1-Nrf2-IN-24 increases the AKR1B10 mRNA expression. Keap1-Nrf2-IN-24 shows good metabolic stability.
    Keap1-Nrf2-IN-24
  • HY-143243
    Antioxidant agent-5
    		Inhibitor
    Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway.
    Antioxidant agent-5
  • HY-N1970R
    5,7-Dihydroxychromone (Standard)
    		Activator
    5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone. This product is intended for research and analytical applications. 5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
    5,7-Dihydroxychromone (Standard)
  • HY-130495
    CDDO-TFEA
    		Activator
    CDDO-TFEA (RTA 404; TP-500) is a trifluoroacetamide derivative of CDDO with enhanced ability to cross the blood-brain barrier. CDDO is an Nrf2 activator that inhibits proliferation and induces differentiation and apoptosis in various cancer cells. CDDO-TFEA can enhance Nrf2 expression and signaling in various neurodegenerative disease models, including those mimicking multiple sclerosis, amyotrophic lateral sclerosis, and Huntington's disease. CDDO-TFEA induces apoptosis and blocks colony formation in Ewing's sarcoma and neuroblastoma cell lines with IC50 values ranging from 85-170 nM.
    CDDO-TFEA
  • HY-W505984
    TPNA10168
    		Activator
    TPNA10168 is an Nrf-2 activator that activates the Keap1-Nrf2-ARE pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases.
    TPNA10168
  • HY-N0823R
    Lithospermic acid (Standard)
    		Activator
    Lithospermic acid (Standard) is the analytical standard of Lithospermic acid. This product is intended for research and analytical applications. Lithospermic acid ((+)-Lithospermic acid) is a plant-derived polycyclic phenolic carboxylic acid isolated from Salvia miltiorrhiza, and has the anti-oxidative and hepatoprotective activity on carbon tetrachloride (CCl4)-induced acute liver damage in vitro and in vivo.
    Lithospermic acid (Standard)
  • HY-W590845
    Ethyl (E)-ferulate
    		Activator
    Ethyl (E)-ferulate is an AMPK/Nrf2 signaling pathway activator that can reduce lipopolysaccharide (HY-D1056)-induced acute lung injury. Additionally, Ethyl (E)-ferulate exhibits free radical scavenging properties, providing anti-inflammatory, antioxidant, neuroprotective, and sunscreen effects. Ethyl (E)-ferulate holds promise for research in the fields of inflammation and neurodegenerative diseases.
    Ethyl (E)-ferulate
  • HY-N2535R
    Coniferaldehyde (Standard)
    		Activator
    Coniferaldehyde (Standard) is the analytical standard of Coniferaldehyde. This product is intended for research and analytical applications. Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities.
    Coniferaldehyde (Standard)
  • HY-115849
    Nrf2-Activator-12G
    		Activator 99.61%
    Nrf2-Activator-12G (compd 12g) is an activator of Nrf2. Nrf2-Activator-12G induces the expression of nrf2-dependentantioxidant enzymes at both mRNA and protein levels in DAergic neuronal cell. Nrf2-Activator-12G can used in study Parkinson’s Disease.
    Nrf2-Activator-12G
  • HY-N0326R
    L-Methionine (Standard)
    		Activator
    L-Methionine (Standard) is the analytical standard of L-Methionine. This product is intended for research and analytical applications. L-Methionine is an L-isomer of orally active Methionine, an essential amino acid. Methionine is a strong liver antidote that acts as a liver protector. L-Methionine can inhibit cell proliferation and induce cell apoptosis. L-Methionine has antitumor and antioxidant activity.
    L-Methionine (Standard)
  • HY-162096
    Keap1-Nrf2-IN-17
    		Inhibitor
    Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of Keap1-Nrf2 protein-protein interaction.
    Keap1-Nrf2-IN-17
  • HY-N12486
    Isofalcarintriol
    		Activator
    Isofalcarintriol is a NRF2 activator and selective inhibitor of the mitochondrial ATP synthase. Isofalcarintriol can be used for aging study.
    Isofalcarintriol
  • HY-N0005R
    Curcumin (Standard)
    		Activator
    Curcumin (Standard) is the analytical standard of Curcumin. This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin (Standard)
  • HY-B1135R
    Benzbromarone (Standard)
    Benzbromarone (Standard) is the analytical standard of Benzbromarone. This product is intended for research and analytical applications. Benzbromarone is an orally active anti-gout agent. Benzbromarone has anti-infammatory, anti-oxidative stress and nephroprotective effects. Benzbromarone can be used for the research of hyperuricemia and gout.
    Benzbromarone (Standard)
  • HY-N0682R
    Pyridoxine (hydrochloride) (Standard)
    Pyridoxine (hydrochloride) (Standard) is the analytical standard of Pyridoxine (hydrochloride). This product is intended for research and analytical applications. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine (hydrochloride) (Standard)
  • HY-B0854R
    Mancozeb (Standard)
    		Activator
    Mancozeb (Standard) is the analytical standard of Mancozeb. This product is intended for research and analytical applications. Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.
    Mancozeb (Standard)
  • HY-138291
    Ethoxyquin dimer
    Ethoxyquin dimer is a dimer of Ethoxyquin (HY-B1425). Ethoxyquin dimer is an antioxidant. Ethoxyquin dimer can more readily accumulate in liver and adipose tissue compared with Ethoxyquin. Ethoxyquin above 10 mg/kg shows hepatotoxicity in mice.
    Ethoxyquin dimer
Cat. No. Product Name / Synonyms Application Reactivity