1. Signaling Pathways
  2. NF-κB
  3. Keap1-Nrf2

Keap1-Nrf2

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-122550
    Artemisitene
    Activator 98.74%
    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-N2535
    Coniferaldehyde
    Activator 99.94%
    Coniferaldehyde (4-Hydroxy-3-methoxycinnamaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells. Coniferaldehyde has antioxidant and anti-inflammatory activities.
    Coniferaldehyde
  • 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-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-N2292
    Kinsenoside
    Activator 99.91%
    Kinsenoside is the main active ingredient of the genus plant, and has various biological activities. Kinsenoside and Nrf2 depend on the protection of nuclear cells (NPCs), which significantly reduces their ability to survive. Kinsenoside Active NPC Medium AKT-ERK1/2-Nrf2 Signal passage, Prevent physical decline, aging, harmonious physical function impairment. Kinsenoside can improve the puncture guide model for intermediate vertebral wall discharge (IDD).
    Kinsenoside
  • 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-145879
    Nrf2 activator-2
    Activator 98.92%
    Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells.
    Nrf2 activator-2
  • HY-N7108
    7-Hydroxyflavone
    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
  • 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-N3075
    Phytol
    Inhibitor ≥98.0%
    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-113848
    AEM1
    Inhibitor 98.99%
    AEM1 is a Nrf2 inhibitor. AEM1 reduces the expressions of Nrf2-dependent genes in A549 cells and inhibits the growth of A549 cells in vitro and in vivo.
    AEM1
  • HY-116152
    Cipepofol
    Activator 99.42%
    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-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 99.63%
    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-16561R
    Resveratrol (Standard)
    Activator 99.73%
    Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-120912
    Gingerenone A
    Activator 99.49%
    Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale.
    Gingerenone A
  • HY-N4113
    Glycycoumarin
    Modulator 99.89%
    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-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-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-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
Cat. No. Product Name / Synonyms Application Reactivity