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-B1051
    Flumethasone
    		Degrader 99.84%
    Flumethasone (Flumetasone) is an orally active, high selective and potent glucocorticoid receptor (GR) agonist. Flumethasone activates GR to inhibit nuclear factor kappa B (NF-κB)-mediated pro-inflammatory cytokine production (TNF-α, IL-1β) and promotes anti-inflammatory gene expression (IL-10), while also regulating metabolic enzyme activity (tyrosine aminotransferase induction). Flumethasone is promising for research of inflammatory diseases, cancer, and endocrine regulation.
    Flumethasone
  • HY-N0106
    (Rac)-Salvianic acid A sodium
    		Activator ≥98.0%
    (Rac)-Salvianic acid A sodium is the racemic form of Salvianic acid A (HY-N1913). Salvianic acid A is an orally active phenolic compound that induces Nrf2/HO-1 activation and inhibits the NF-κB pathway, and it also activates the mitochondrial antioxidant defense system (Mitochondrial Metabolism). Salvianic acid A exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties (Apoptosis), demonstrating potential for research into inflammation and cardiovascular diseases.
    (Rac)-Salvianic acid A sodium
  • HY-146086
    Nrf2 activator-4
    		Activator 98.03%
    Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model.
    Nrf2 activator-4
  • HY-N0818
    Chikusetsusaponin Iva
    		Inhibitor 98.95%
    Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects.
    Chikusetsusaponin Iva
  • HY-133114
    Ezetimibe ketone
    		Activator 99.97%
    Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.
    Ezetimibe ketone
  • HY-131592
    Tricetin
    		Inhibitor 99.19%
    Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway.
    Tricetin
  • HY-N1902S
    4-Hydroxyphenylacetic acid-d6
    		Activator 99.16%
    4-Hydroxyphenylacetic acid-d6 is the deuterium labeled 4-Hydroxyphenylacetic acid. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2.
    4-Hydroxyphenylacetic acid-d<sub>6</sub>
  • HY-N6866
    Gomisin N
    		Activator 99.94%
    Gomisin N is an orally active lignan compound. Gomisin N can be isolated from Schisandra chinensis. Gomisin N induces Apoptosis in a variety of cells. Gomisin N activates AMPK, Akt, MAPK/ERK, Nrf2, caspase-3 and PARP-1. Gomisin N inhibits GSK3β, nitric oxide (NO), and proinflammatory cytokines (IL-1β, IL-6, TNF-α). Gomisin N has anti-inflammatory, antioxidant, anti-obesity, anti-diabetic, and anti-melanogenesis activities. Gomisin N has anti-tumor activity against cervical cancer and liver cancer. Gomisin N improves Alzheimer's disease.
    Gomisin N
  • HY-Z0548
    Methyl 3,4-dihydroxybenzoate
    		Agonist 99.88%
    Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect.
    Methyl 3,4-dihydroxybenzoate
  • HY-B0854
    Mancozeb
    		Activator
    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
  • HY-144634
    DDO-7263
    		Activator 99.83%
    DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD).
    DDO-7263
  • HY-N6641
    Monascin
    		Activator 99.79%
    Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist.
    Monascin
  • HY-101140A
    KI696 isomer
    		Inhibitor 99.32%
    KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
    KI696 isomer
  • HY-16561S
    Resveratrol-d4
    		Activator 99.36%
    Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
    Resveratrol-d<sub>4</sub>
  • HY-N1970
    5,7-Dihydroxychromone
    		Activator 99.94%
    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
  • HY-W014841
    Sodium hippurate, 98%
    		Inhibitor 99.91%
    Sodium hippurate, 98% is an orally active metabolite. Sodium hippurate, 98% can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Sodium hippurate, 98% decreases NRF2, MMP9 and leads to ROS accumulation. Sodium hippurate, 98% activates TGFβ/SMAD signaling. Sodium hippurate, 98% improves hyperuricemia and colitis. Sodium hippurate, 98% can also be used in cardiovascular disease research. .
    Sodium hippurate, 98%
  • HY-W009356
    L-Cystine hydrochloride
    		Activator ≥98.0%
    L-Cystine hydrochloride is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine hydrochloride elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-Cystine hydrochloride reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine hydrochloride combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine hydrochloride is promising for research of cystinuria and kidney stones
    L-Cystine hydrochloride
  • HY-153873
    MSU38225
    		Inhibitor 99.52%
    MSU38225 is an Nrf-2 inhibitor that increases levels of reactive oxygen species (ROS). MSU38225 inhibits the growth of human lung cancer cells and enhances the sensitivity of human lung cancer cells to chemotherapy in vitro and in vivo. MSU38225 can be used in cancer research.
    MSU38225
  • HY-N7617
    Toralactone
    		Inhibitor 98.75%
    Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
    Toralactone
  • HY-N0449
    Nordihydrocapsaicin
    		Modulator 99.82%
    Nordihydrocapsaicin, an analog of Capsaicin (HY-10448), is an orally active compound with pungent properties and anti-cancer activities, which is found in fresh and processed peppers. Nordihydrocapsaicin can cause a burning sensation when consumed.
    Nordihydrocapsaicin
Cat. No. Product Name / Synonyms Application Reactivity