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-12213
    CDDO-EA
    		Activator 99.71%
    CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
    CDDO-EA
  • HY-N0826
    Corynoline
    		Activator 99.12%
    Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits anti-inflammatory activity by activating Nrf2.
    Corynoline
  • 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-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-113848
    AEM1
    		Inhibitor 98.99%
    AEM1 is an Nrf2 inhibitor with anti-tumor and oral activity. AEM1 promotes the differentiation of HepaRG cells towards mature liver cells, aiding in the recovery of damaged liver.
    AEM1
  • 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-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 98.53%
    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-100375
    Diroximel fumarate
    		Activator 99.90%
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity.
    Diroximel fumarate
  • HY-N3075
    Phytol
    		Inhibitor 98.93%
    Phytol ((E)-Phytol) is an orally active diterpenoid alcohol that can be extracted from chlorophyll. Phytol has antioxidant, anti-inflammatory, anti-schistosomiasis and antibacterial activities.
    Phytol
  • HY-153340
    I-152
    		Activator 98.78%
    I-152 is a conjugate containing N-acetyl-cysteine (NAC) and cysteamine (MEA). I-152 activates NRF2 and ATF4 signals. I-152 has anti-proliferative properties.
    I-152
  • HY-112671
    CDDO-dhTFEA
    		Activator 99.71%
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
    CDDO-dhTFEA
  • 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-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-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-145532
    S-Allylmercaptocysteine
    		Activator
    S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-allylmercaptocysteine achieves its anti-cancer effect through a variety of pathways such as inducing the apoptosis of cancer cells through the TGF-β signaling pathway, or reducing the NF-κB activity and up-regulating Nrf2 to achieve the effects of anti-inflammation and anti-oxidation.
    S-Allylmercaptocysteine
  • 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-N0818
    Chikusetsusaponin Iva
    		Inhibitor 98.95%
    Chikusetsusaponin Iva is the main active component of triterpenoid saponins, acts as an activator of protein kinases, and has a resistance effect against thrombosis and some metabolic diseases.
    Chikusetsusaponin Iva
  • HY-162307
    Nrf2 degrader 1
    		Degrader
    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-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
Cat. No. Product Name / Synonyms Application Reactivity