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-N6653
    Lentinan
    		Activator
    Lentinan is an orally active biocompatible multifunctional polysaccharide with biological activities such as anti-inflammatory, antioxidant, immune regulation, anti-tumor, hypoglycemic, and lipid-lowering[1][4].
    Lentinan
  • HY-N0509
    Astilbin
    		Activator 99.80%
    Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
    Astilbin
  • HY-N0823
    Lithospermic acid
    		Activator 99.56%
    Lithospermic acid ((+)-Lithospermic acid) is a plant-derived polycyclic phenolic carboxylic acid isolated from Salvia miltiorrhiza, and has the anti-oxidative and hepatoprotective activity on carbon tetrachloride (CCl4)-induced acute liver damage in vitro and in vivo.
    Lithospermic acid
  • HY-B2230
    Hinokitiol
    		Inhibitor 99.83%
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
    Hinokitiol
  • HY-N0682
    Pyridoxine hydrochloride
    		99.96%
    Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine hydrochloride
  • HY-Y1325I
    Sodium acetate trihydrate, 99.5%
    		Activator 99.99%
    Sodium acetate trihydrate, 99.5% is a short-chain fatty acid salt with multiple biological activities. Sodium acetate trihydrate, 99.5% serves as a direct precursor of acetyl-CoA, and it extensively affects gene expression by promoting histone acetylation. Sodium acetate trihydrate, 99.5% can activate the p38 MAPK pathway to induce cancer cell apoptosis. Sodium acetate trihydrate, 99.5% can activate the Wnt/β-catenin signaling pathway to stimulate the proliferation and migration of cecal epithelial cells, thereby improving intestinal health. Sodium acetate trihydrate, 99.5% alleviates lead accumulation and oxidative damage by upregulating the testosterone-dependent eNOS/NO/cGMP signaling pathway, as well as activating the Nrf2/HO-1 pathway and its downstream antioxidant enzymes.
    Sodium acetate trihydrate, 99.5%
  • HY-12519
    Oltipraz
    		Activator 99.87%
    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
  • HY-16561R
    Resveratrol (Standard)
    		Activator
    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-113298
    Citraconic acid
    		Inhibitor 99.08%
    Citraconic acid (Methylmaleic acid) is an orally active inhibitor targeting the NLRP3 inflammasome and Keap1-Nrf2 pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052).
    Citraconic acid
  • HY-N0147
    Rutaecarpine
    		Activator 99.09%
    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
  • 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-N0638
    Dendrobine
    		Activator 99.92%
    Dendrobine is an alkaloid isolated from Dendrobium nobile. Dendrobine possesses antiviral activity against influenza A viruses, with IC50s of 3.39 μM, 2.16 μM and 5.32 μM for A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2), respectively. Dendrobine activates the JNK/p38/Nrf2 signaling pathway. Dendrobine exhibits antiviral, antitumor, anti-inflammatory, and neuroprotective properties.
    Dendrobine
  • HY-W001083
    3-Hydroxyphenylacetic acid
    		Activator 99.77%
    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-N0005R
    Curcumin (Standard)
    		Activator
    Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin (Standard)
  • HY-113556
    Sappanone A
    		Activator 99.87%
    Sappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular .
    Sappanone A
  • HY-101025
    Nrf2-IN-1
    		Inhibitor 99.88%
    Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML).
    Nrf2-IN-1
  • HY-129960
    L-Selenocystine
    		Inhibitor 98.0%
    L-Selenocystine is a selenium-containing amino acid. L-Selenocystine has redox properties. L-Selenocystine is cytotoxic to various tumor cells and can induce the production of ROS and apoptosis. L-Selenocystine can block the Nrf2 and autophagy pathways. L-Selenocystine has anti-tumor activity.
    L-Selenocystine
  • HY-162307
    Nrf2 degrader 1
    		Degrader 99.12%
    Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC50 of 0.1-1 μM in huH1 cells. 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 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer.
    Nrf2 degrader 1
  • HY-19734
    NK-252
    		Activator 99.74%
    NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
    NK-252
  • 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
Cat. No. Product Name / Synonyms Application Reactivity