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-W009203
    L-Cystine dihydrochloride
    		Activator ≥98.0%
    L-Cystine dihydrochloride is the dihydrochloride salt form of L-Cystine (HY-N0394). L-Cystine dihydrochloride elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-cystine dihydrochloride reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine dihydrochloride 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 dihydrochloride is promising for research of cystinuria and kidney stones
    L-Cystine dihydrochloride
  • HY-129225
    WRR139
    		Inhibitor 99.71%
    WRR139 is a peptide vinyl sulfone involving in disease processes such as inflammation and cancer. WRR139 is also a cytosolic enzyme N-glycanase 1 (NGLY1) and Nrf1 inhibitor. WRR139 enhances Carfilzomib cytotoxicity against cancer cells.
    WRR139
  • HY-122550
    Artemisitene
    		Activator 99.93%
    Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability.
    Artemisitene
  • HY-13755A
    (R)-Sulforaphane
    		Activator 99.48%
    (R)-Sulforaphane (L-Sulforaphane) is a orally active, potent inducer of the Keap1/Nrf2/ARE pathway, exhibiting antioxidant and anticancer activities. (R)-Sulforaphane primarily functions by upregulating phase II detoxifying enzymes in cells, aiding in the removal of carcinogens and combating oxidative stress. (R)-Sulforaphane is capable of modulating gene expression, influencing various signaling pathways, including Nrf2, NF-κB, and AP-1. (R)-Sulforaphane can be used in studies of tumor biology, antioxidant defense mechanisms, as well as inflammation and immune responses.
    (R)-Sulforaphane
  • HY-W250116
    Co(III) protoporphyrin IX chloride
    		Inducer
    Co(III) protoporphyrin IX chloride (Protoporphyrin IX cobaltic chloride) is an inducer of HO-1. Co(III) protoporphyrin IX chloride has activities such as anti-inflammation and antibacterial properties. Co(III) protoporphyrin IX chloride can also be used in the research of ischemia-reperfusion injury models.
    Co(III) protoporphyrin IX chloride
  • HY-N7088
    Raffinose
    		Activator ≥98.0%
    Raffinose (Melitose) regulates intestinal flora, inhibits TLR4-MyD88-NF-κB signaling pathway, and activates Nrf2 signaling pathway. Raffinose exhibits anti-inflammatory, antioxidant, and immunomodulatory activities. Raffinose is orally active.
    Raffinose
  • HY-W001083
    3-Hydroxyphenylacetic acid
    		Activator 99.03%
    3-Hydroxyphenylacetic acid is an orally active flavonoid metabolite produced by intestinal flora, with blood pressure-lowering activity. 3-Hydroxyphenylacetic acid can also inhibit ferroptosis by upregulating the expression of GPX4, thereby improving spermatogenic dysfunction in aged mice. In addition, abnormal levels of 3-Hydroxyphenylacetic acid are closely related to certain diseases, such as autism spectrum disorders.
    3-Hydroxyphenylacetic acid
  • HY-162307
    Nrf2 degrader 1
    		Degrader 99.12%
    Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer effects. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively.
    Nrf2 degrader 1
  • HY-N0162R
    Luteolin (Standard)
    		Inhibitor 98.71%
    Luteolin (Standard) is the analytical standard of Luteolin. This product is intended for research and analytical applications. Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
    Luteolin (Standard)
  • HY-W009731
    Dibenzoylmethane
    		Activator ≥98.0%
    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
  • HY-103435
    Vialinin A
    		Activator 99.90%
    Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke.
    Vialinin A
  • HY-116152
    Cipepofol
    		Activator 99.82%
    Cipepofol (Ciprofol), a novel 2,6-disubstituted phenol derivative, is a positive allosteric modulator and direct agonist of the GABAA receptor. Cipepofol can cause the central nerve inhibition and promote sleep based on the structural modification of Propofol (HY-B0649). Cipepofol can activate the sirtuin1 (Sirt1)/Nrf2 pathway. Cipepofol protects the heart against Isoproterenol (ISO; HY-B0468)-induced myocardial infarction by reducing cardiac oxidative stress, inflammatory response and cardiomyocyte apoptosis.
    Cipepofol
  • HY-100618
    Hispidin
    		99.94%
    Hispidin, a PKC inhibitor and a phenolic compound can be found in Phellinus linteus, has been shown to possess strong anti-oxidant, anti-cancer, anti-diabetic, and anti-dementia properties.
    Hispidin
  • HY-N0440
    Germacrone
    		Activator 99.76%
    Germacrone is a sesquiterpene compound with multiple biological activities. Germacrone inhibits the H1N1 and H3N2 influenza A virus and the influenza B virus. Germacrone blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone inhibits 5α-reductase and has anti-androgenic effect. Germacrone has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone also has antioxidant activity.
    Germacrone
  • HY-P9928A
    Alirocumab (anti-PCSK9)
    		98.24%
    Alirocumab (anti-PCSK9) is an anti-PCSK9 human monoclonal antibody. Alirocumab (anti-PCSK9) inhibits PCSK9. Alirocumab (anti-PCSK9) reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab (anti-PCSK9) increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab (anti-PCSK9) improves atherosclerosis and inflammation.
    Alirocumab (anti-PCSK9)
  • HY-N4113
    Glycycoumarin
    		Modulator 99.98%
    Glycycoumarin is a potent antispasmodic agent. Glycycoumarin is a major bioactive coumarin of licorice and exhibits antispasmodic activity. Glycycoumarin also has hepatoprotective effect. Glycycoumarin can be used for the research of abdominal pain and liver diseases.
    Glycycoumarin
  • HY-N0807
    Swertiamarin
    		Modulator 99.03%
    Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis.
    Swertiamarin
  • HY-N7108
    7-Hydroxyflavone
    		Inhibitor 99.84%
    7-Hydroxyflavone is a flavonoid isolated from Clerodendrum phlomidis, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway. 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM. 7-Hydroxyflavone inhibits COX-2 and 5-LOX with IC50 of 27 µg/mL and 33 µg/mL. 7-Hydroxyflavone is orally active.
    7-Hydroxyflavone
  • HY-149508
    Nrf2-IN-3
    		Inhibitor 99.19%
    Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
    Nrf2-IN-3
  • HY-12213
    CDDO-EA
    		Activator 99.78%
    CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
    CDDO-EA
Cat. No. Product Name / Synonyms Application Reactivity