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-N15660
    Azafrin
    		Activator
    Azafrin, a carotenoid, is one of the most abundant active ingredients in C. grandiflora. Azafrin increases HO-1, NQO1, and Nrf2 expression. Azafrin shows cardioprotective effect against myocardial injury via activation of the Nrf2-ARE pathway. Azafrin can be used for research of cardiovascular diseases.
    Azafrin
  • HY-120825
    QD 232
    		Activator
    QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model.
    QD 232
  • HY-110067
    VO-OHPic
    		Activator
    VO-OHPic is a reversible, noncompetitive PTEN inhibitor with an human IC50 value of 46 nM. VO-OHPic inhibits PTEN signaling, activates Akt-GSK3β and Nrf-2/HO-1 pathways, induces apoptosis resistance and elevates IL-10 levels. VO-OHPic inhibits autophagy, ferroptosis and oxidative stress. VO-OHPic can be used for the research of acute myocardial infarction, intervertebral disc degeneration, cardiomyopathy and cancer.
    VO-OHPic
  • HY-N16929
    Gymnoside II
    		Activator
    Gymnoside II is one of the main bioactive constituents isolated from Bletilla striata. Gymnoside II inhibits nano SiO2-induced A549 cell viability reduction, apoptosis, and ROS generation by activating Nrf2. Gymnoside II upregulates HO-1 and γ-GCSc, while downregulating the Bax/Bcl-2 ratio. Gymnoside II is applicable for research on nano SiO2-induced pulmonary injury.
    Gymnoside II
  • HY-146168
    Nrf2 activator-5
    		Activator
    Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities.
    Nrf2 activator-5
  • HY-12519S
    Oltipraz-d3
    		Activator
    Oltipraz-d3 is the deuterium labeled Oltipraz. Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
    Oltipraz-d<sub>3</sub>
  • HY-183692
    FXR agonist 18
    		Activator
    FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.
    FXR agonist 18
  • HY-N0147R
    Rutaecarpine (Standard)
    		Activator
    Rutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine (Standard)
  • HY-N3121R
    Pachypodol (Standard)
    		Activator
    Pachypodol (Standard) is the analytical standard of Pachypodol (HY-N3121). This product is intended for research and analytical applications. Pachypodol is an orally active methoxyflavonoid compound. Pachypodol activates the ERK-dependent Nrf2 pathway and inhibits Apoptosis. Pachypodol exhibits activities such as antioxidant, cytoprotective, anti-inflammatory effects. Pachypodol improves cognition. Pachypodol exerts protective effects against cardiac and liver damage. Pachypodol has anticancer activity against colon cancer.
    Pachypodol (Standard)
  • HY-12519G
    Oltipraz (GMP)
    		Activator
    Oltipraz (GMP) is Oltipraz (HY-12519) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Oltipraz has an inhibitory effect on HIF-1α activation. Oltipraz is a potent Nrf2 activator.
    Oltipraz (GMP)
  • HY-B0298AR
    Clemastine fumarate (Standard)
    		Activator
    Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine 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 (Standard)
  • HY-163772
    Fraxinellone analog 1
    		Activator
    Fraxinellone analog 1 (compound 2) is a potent and rapid activator of the Nrf2 mediated antioxidant defense system, which protects against glutamate-mediated excitotoxicity and induces the expression of antioxidant genes Gpx4, Sod1, and Nqo1. Fraxinellone analog 1 has neuroprotective effects and regulatory effects against oxidative stress and inflammation, and can be used in the study of neurodegenerative diseases.
    Fraxinellone analog 1
  • HY-180529
    4-Octyl itaconate-Bn-S-NH2
    		Activator
    4-Octyl itaconate-Bn-S-NH2 (Compound 8b) is a vasodilator. 4-Octyl itaconate-Bn-S-NH2 can slowly and stably release H₂S, and it alleviates oxidative stress through an antioxidant reaction that depends on the activation of Nrf2. 4-Octyl itaconate-Bn-S-NH2 inhibits the production of intracellular ROS caused by H₂O₂ damage and the cytotoxicity of cells, and activates potassium channel. 4-Octyl itaconate-Bn-S-NH2 can be used for research on hypertension.
    4-Octyl itaconate-Bn-S-NH2
  • HY-W772717
    L-Cystine disodium monohydrate
    		Activator
    L-Cystine disodium monohydrate is an orally active extracellular form of L-Cysteine (HY-Y0337), occurring in proteins of plants and animals. L-Cystine disodium monohydrate elevates Nrf2 protein expression and activates Nrf2 transcription factor. L-Cystine disodium monohydrate reduces ROS generation and protects against oxidant- or Doxorubicin (HY-15142A)-induced apoptosis. L-Cystine disodium monohydrate 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 disodium monohydrate is promising for research of cystinuria and kidney stones.
    L-Cystine disodium monohydrate
  • HY-16561S1
    Resveratrol-13C6
    		Activator
    Resveratrol-13C6 is the 13C-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-<sup>13</sup>C<sub>6</sub>
  • HY-107736
    AI-3
    		Activator
    AI-3 is a potent ARE (antioxidant response element) activator. AI-3 increases the NQO1 at the transcript levels and protein expression levels. AI-3 has the potential for the research of oxidative stress related diseases.
    AI-3
  • HY-175270
    MAGL-IN-22
    		Activator
    MAGL-IN-22 (Compound 40) is a reversible, competitive, selective and BBB-penetrable MAGL inhibitor with an IC50 of 0.34  μM for hMAGL. MAGL-IN-22 has significant antioxidant and anti-inflammatory activity, and activates the Nrf2 pathway and significantly inhibits NFκB-mediated inflammation, without inducing cytotoxic effects. MAGL-IN-22 can be used for neurodegenerative diseases, chronic pain and cancers research.
    MAGL-IN-22
  • HY-151431
    Nrf2/HO-1 activator 2
    		Activator
    Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD).
    Nrf2/HO-1 activator 2
  • HY-180155
    Keap1/Nrf2/ARE activator 2
    		Activator
    Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease.
    Keap1/Nrf2/ARE activator 2
  • HY-156081
    Nrf2 activator-9
    		Activator
    Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis.
    Nrf2 activator-9
Cat. No. Product Name / Synonyms Application Reactivity