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-139408
    17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid
    		Activator
    17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid (17-Oxo-DHA) is a metabolite of lipoxygenase-mediated oxidation of DHA. 17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid is a PPARγ agonist and activates a Nrf2 dependent antioxidant reaction.
    17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid
  • HY-N0637R
    Eriodictyol (Standard)
    		Activator
    Eriodictyol (Standard) is the analytical standard of Eriodictyol. This product is intended for research and analytical applications. Eriodictyol is a flavonoid isolated from the Chinese herb, with antioxidant and anti-inflammatory activity. Eriodictyol induces Nrf2 signaling pathway. Eriodictyol is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 18 nM.
    Eriodictyol (Standard)
  • HY-Z0548S1
    Methyl 3,4-dihydroxybenzoate-d3-1
    		Agonist
    Methyl 3,4-dihydroxybenzoate-d3-1 is the deuterium labeled Methyl 3,4-dihydroxybenzoate. 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[1].
    Methyl 3,4-dihydroxybenzoate-d<sub>3</sub>-1
  • HY-124834
    Nrf2 activator-10
    		Activator
    Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent inducer for antioxidant response element (ARE) (EC50 is 2.7 μM) and an activator for Nrf2. Nrf2 activator-10 modifies Keap1, blocks Cul3-Keap1 ubiquitin ligase complex, activates the transcription of Nrf2. Nrf2 activator-10 protects cells from H2O2-induced apoptosis.
    Nrf2 activator-10
  • HY-156065
    S217879
    		Activator
    S217879 is a highly potent and selective NRF2 activator. S217879 disrupts the KEAP1-NRF2 interaction leading to robust NRF2 pathway activation. S217879 can be used for non-alcoholic steatohepatitis (NASH) research.
    S217879
  • HY-122946
    Pterisolic acid B
    Pterisolic acid B (Compound 2) is an ent-Kaurane diterpenoid. Pterisolic acid B can be isolated from fern Pteris semipinnata (Pteridaceae).
    Pterisolic acid B
  • HY-N0682S2
    Pyridoxine-d5 hydrochloride
    Pyridoxine-d5 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride[1]. 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[2].
    Pyridoxine-d<sub>5</sub> hydrochloride
  • HY-N0682S1
    Pyridoxine-d2 hydrochloride
    Pyridoxine-d2 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride 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-d<sub>2</sub> hydrochloride
  • HY-N0290R
    Mangiferin (Standard)
    		Activator
    Mangiferin (Standard) is the analytical standard of Mangiferin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-125129
    Carlinoside
    Carlinoside is a flavone glycoside with hepatoprotective efficiency. Carlinoside reduces hepatic bilirubin accumulation by stimulating bilirubin-UGT activity through Nrf2 gene expression. Carlinoside has the potential to intervene hyperbilirubinemia due to liver dysfunction.
    Carlinoside
  • HY-B1328R
    Pyridoxine (Standard)
    Pyridoxine (Standard) is the analytical standard of Pyridoxine. This product is intended for research and analytical applications. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway. In Vitro: Pyridoxine exerts a protective potential against AD, attenuates ROS levels, decreases the expressions of cytoplasmic Nrf2, and upregulates whole-cell HO-1 expression.
    Pyridoxine (Standard)
  • HY-141439
    TBE 31
    		Activator
    TBE 31 is a potent and orally active NQO1 inducer with an Dm value of 1.1 nM. TBE 31 also is a potent Nrf2 activator. TBE 31 reacts with cysteines of Keap1, impairing its ability to target nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) for degradation. TBE 31 shows cytoprotective effects.
    TBE 31
  • HY-168709
    Nrf2 activator 18
    		Activator
    Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC50 of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model.
    Nrf2 activator 18
  • HY-124941
    7-Deacetylgedunin
    		Activator
    7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro.
    7-Deacetylgedunin
  • HY-N0106R
    (Rac)-Salvianic acid A (sodium) (Standard)
    		Activator
    (Rac)-Salvianic acid A (sodium) (Standard) is the analytical standard of (Rac)-Salvianic acid A (sodium). This product is intended for research and analytical applications. (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) (Standard)
  • HY-168065
    Keap1-Nrf2-IN-22
    		Inhibitor
    Keap1-Nrf2-IN-22 (compound 19) is a Keap1-Nrf2 inhibitor， with a KD2 value of 42.2 nM for Keap1. Keap1-Nrf2-IN-22 can be used for the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury.
    Keap1-Nrf2-IN-22
  • HY-N0826R
    Corynoline (Standard)
    		Activator
    Corynoline (Standard) is the analytical standard of Corynoline. This product is intended for research and analytical applications. 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 (Standard)
  • HY-W083376A
    4-Methoxychalcone-1
    		Inhibitor
    4-Methoxychalcone is a naturally occurring chalcone compound. 4-Methoxychalcone has antioxidant activity, anti-inflammatory activity, antitumor activity and antibacterial activity. 4-Methoxychalcone can be used to study inflammation and tumor models.
    4-Methoxychalcone-1
  • HY-162170
    Anti-inflammatory agent 72
    		Activator
    Anti-inflammatory agent 72 (compound 5) is a novel resveratrol derivative hybrid with benzoylhydrazine. Anti-inflammatory agent 72 shows anti-inflammatory and antioxidant activities by activating Nrf2 and inhibiting NF-κB p65/iNOS and MAPKs signaling pathways.
    Anti-inflammatory agent 72
  • HY-N15190
    Sesaminol
    		Activator
    Sesaminol is an orally active activator for Nrf2-ARE pathway, that promotes the the nuclear translocation of Nrf2 and enhances the NQO1 expression, thereby enhances the cell's defense against oxidative stress. Sesaminol inhibits 6-OHDA (HY-B1081)-induced ROS production and apoptosis in cell SH-SY5Y. Sesaminol exhibits neuroprotective efficacy against Rotenone (HY-B1756)-induced Parkinson's disease.
    Sesaminol
Cat. No. Product Name / Synonyms Application Reactivity