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-14909
    Bardoxolone
    		Activator 99.50%
    Bardoxolone (CDDO; RTA 401) is a Nrf2 activator. Bardoxolone shows anti-SARS-CoV-2 3CLpro with IC50 of 27.99 μM. Bardoxolone activates the Nrf2 pathway and inhibits the NF-κB pathway. Bardoxolone can induce cells differentiation, apoptosis and shows antiproliferative activity against cancer cells. Bardoxolone can increase ROS and decrease intracellular GSH levels. Bardoxolone inhibits Z-VAD-FMK (HY-16658B)-induced necroptosis. Bardoxolone can be used for the research of cancer, inflammation and infection, such as SARS-CoV infection and glioblastoma.
    Bardoxolone
  • HY-N0680
    Thiamine hydrochloride
    		Activator 99.97%
    Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.Thiamine hydrochloride activates NrF-2/HO-1 and inhibits TLR4, NF-κB. Thiamine hydrochloride has neuroprotective and anti-inflammatory effects. Thiamine hydrochloride can be used in the studys of diabetic complications, neurological diseases, cancers, and colitis.
    Thiamine hydrochloride
  • HY-B1135
    Benzbromarone
    		99.91%
    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
  • HY-B0298A
    Clemastine fumarate
    		Activator 99.96%
    Clemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine fumarate
  • HY-N0643
    Carnosol
    		Activator 99.90%
    Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
    Carnosol
  • HY-W016562
    Hippuric acid
    		Inhibitor 99.98%
    Hippuric Acid is an orally active metabolite. Hippuric Acid can be produced by intestinal microorganisms from the metabolism of polyphenols, benzoic acid. Hippuric Acid decreases NRF2, MMP9 and leads to ROS accumulation. Hippuric Acid activates TGFβ/SMAD signaling. Hippuric Acid improves hyperuricemia and colitis. Hippuric Acid can also be used in cardiovascular disease research. .
    Hippuric acid
  • HY-N0394
    L-Cystine
    		Activator 99.84%
    L-Cystine is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-cystine reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine 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 is promising for research of cystinuria and kidney stones
    L-Cystine
  • HY-B1328
    Pyridoxine
    		99.98%
    Pyridoxine (Pyridoxol) is one of the components of vitamin B6. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine
  • HY-N1913
    Danshensu
    		Activator 99.90%
    Danshensu (Dan shen suan A), an orally active phenolic compound, can induce Nrf2/HO-1 activation and inhibition of NF-κB pathway. Danshensu reduces reactive oxygen species (ROS) production, upregulates antioxidant defense mechanism and inhibits intrinsic apoptotic pathway. Danshensu displays a potent antiviral activity against SARS-CoV-2 with EC50 of 0.97 μM. Danshensu has anti-oxidation, anti-apoptosis, anti-lung inflammatory and has the potential for COVID-19, cardiovascular and cerebrovascular diseases research.
    Danshensu
  • HY-N0290
    Mangiferin
    		Activator 99.92%
    Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities.
    Mangiferin
  • HY-B1000
    Selenomethionine
    		Activator 99.86%
    Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity.
    Selenomethionine
  • HY-120912
    Gingerenone A
    		Activator 99.95%
    Gingerenone A is an Nrf2-Gpx4 activator that can induce Ferroptosis in liver damage with oral activity. Gingerenone A has anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging effects in mice.
    Gingerenone A
  • HY-159641
    VVD-130037
    		Activator 99.91%
    VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors.
    VVD-130037
  • HY-N0568
    Madecassoside
    		Activator 99.58%
    Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
    Madecassoside
  • HY-N1902
    4-Hydroxyphenylacetic acid
    		Activator 99.96%
    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
  • HY-110258
    ML334
    		Activator 99.76%
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
    ML334
  • HY-134205A
    CBR-470-1
    		Activator 98.02%
    CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade.
    CBR-470-1
  • HY-N0787
    Cryptochlorogenic acid
    		Activator 99.87%
    Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response.
    Cryptochlorogenic acid
  • HY-P9928
    Alirocumab
    Alirocumab is an anti-PCSK9 human monoclonal antibody. Alirocumab inhibits PCSK9. Alirocumab reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab improves atherosclerosis and inflammation.
    Alirocumab
  • HY-15725
    CDDO-Im
    		Activator 99.30%
    CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
    CDDO-Im
Cat. No. Product Name / Synonyms Application Reactivity