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. 상품명 효과 Purity Chemical Structure
  • HY-N2535R
    Coniferaldehyde (Standard)
    		Activator
    Coniferaldehyde (Standard) is the analytical standard of Coniferaldehyde. This product is intended for research and analytical applications. 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 (Standard)
  • HY-183905
    KR-67607
    		Activator
    KR-67607 is a selective 11β-HSD1 inhibitor, with an IC50 value of 4.8 nM against h11β-HSD1 and 7.1 nM against mouse 11β-HSD1. KR-67607 inhibits stress-induced Glucocorticoid receptor nuclear translocation, reduces cortisol levels, suppresses the expression of ROS and proinflammatory cytokines, and enhances Nrf-2-mediated antioxidant gene transcription. KR-67607 maintains trabecular meshwork structure and reverses elevated intraocular pressure. KR-67607 improves ocular antioxidant activity and mucus secretion, reverses ocular surface damage, and prevents ischemia-reperfusion induced ocular injury. KR-67607 can be used in research related to glaucoma and dry eye disease.
    KR-67607
  • HY-N0606R
    Ginsenoside Rh3 (Standard)
    		Activator
    Ginsenoside Rh3 (Standard) is the analytical standard of Ginsenoside Rh3. This product is intended for research and analytical applications. Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.
    Ginsenoside Rh3 (Standard)
  • HY-B1065R
    Aceglutamide (Standard)
    		Activator
    Aceglutamide (α-N-Acetyl-L-glutamine; N2-Acetylglutamine) (Standard) is the analytical standard of Aceglutamide (HY-B1065). This product is intended for research and analytical applications. Aceglutamide (α-N-Acetyl-L-glutamine; N2-Acetylglutamine) is a neuroprotectant that can penetrate the blood-brain barrier. Aceglutamide can enhance the antioxidant systems of glutathione (GSH), thioredoxin (Trx) and Nrf2. Aceglutamide also inhibits ASK1 and TRAF1, activates the Akt/Bcl-2 anti-apoptotic pathway, enhances the activity of antioxidant enzymes and reduces oxidative damage. Aceglutamide can improve neurological deficits after cerebral ischemia, reduce infarct volume, and inhibit neuronal apoptosis, especially substantia nigra dopaminergic neurons. Aceglutamide can reduce cerebral ischemia/reperfusion injury, improve motor dysfunction, and is used in ischemic stroke-related research.
    Aceglutamide (Standard)
  • HY-N8160
    Dehydrocurdione
    		Activator
    Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity.
    Dehydrocurdione
  • HY-N0005S1
    Curcumin-d3
    		Activator
    Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). 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-d<sub>3</sub>
  • HY-N12486
    Isofalcarintriol
    		Activator
    Isofalcarintriol is a NRF2 activator and selective inhibitor of the mitochondrial ATP synthase. Isofalcarintriol can be used for aging study.
    Isofalcarintriol
  • HY-185185
    S58 aptamer
    		Activator
    S58 aptamer is a ssDNA aptamer targeting transforming growth factor-beta receptor II (TGF-β RII). S58 aptamer inhibits the TGF-β RII interaction with TGF-β. S58 aptamer effectively improves glaucoma filtration surgery (GFS) surgical outcomes by activating the intracellular antioxidant defense PI3K/Akt/Nrf2 signaling pathway.
    S58 aptamer
  • HY-N0260R
    Epmedin C (Standard)
    		Activator
    Epmedin C (Standard) is the analytical standard of Epmedin C. This product is intended for research and analytical applications. Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia.
    Epmedin C (Standard)
  • HY-N0806R
    Sweroside (Standard)
    		Activator
    Sweroside (Standard) is the analytical standard of Sweroside (HY-N0806). This product is intended for research and analytical applications. Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields.
    Sweroside (Standard)
  • HY-133114R
    Ezetimibe ketone (Standard)
    		Activator
    Ezetimibe ketone (Standard) is the analytical standard of Ezetimibe ketone (HY-133114). This product is intended for research and analytical applications. Ezetimibe ketone is an orall active Nrf2 activator and ROS inhibitor. Ezetimibe ketone attenuates H2O2-induced reactive oxygen species production and reduces H2O2-induced apoptosis in renal tubular epithelial cells. Ezetimibe ketone suppresses renal tubular injury and inflammation.
    Ezetimibe ketone (Standard)
  • HY-14909R
    Bardoxolone (Standard)
    		Activator
    Bardoxolone (Standard) is the analytical standard of Bardoxolone (HY-14909). This product is intended for research and analytical applications. Bardoxolone is an orally active activator of nuclear regulatory factor (NRf-2) and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone inhibits SARS-CoV-2 3CL protease with an EC50 value of 0.43 μM in vero cells. Bardoxolone also inhibits necroptosis in HT-29 cells with an EC50 value of 1.30 μM by blocking necrosome formation through inhibiting phosphorylation of RIPK1 and RIPK3. Bardoxolone can be used in research on COVID-19, TNF-induced systemic inflammatory response syndrome (SIRS), and cerebral ischemia-reperfusion injury.
    Bardoxolone (Standard)
  • HY-12519R
    Oltipraz (Standard)
    		Activator
    Oltipraz (Standard) is the analytical standard of Oltipraz. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N16435
    Plumericin
    		Activator
    Plumericin is an anti-inflammatory, antioxidant, and antibacterial agent. Plumericin reduces Apoptosis, promotes Nrf-2 and inhibits NF-κB and AhR activation, blocks STAT3 signaling. Plumericin inhibits Mycobacterium tuberculosis growth. Plumericin can be used for the research of chronic kidney disease, vascular diseases, inflammatory bowel diseases, peritonitis, and tuberculosis.
    Plumericin
  • HY-N0481R
    Roburic acid (Standard)
    		Activator
    Roburic acid (Standard) is the analytical standard of Roburic acid. This product is intended for research and analytical applications. Roburic acid acts as an anti-inflammatory, anti-tumor and osteoclastogenesis inhibitor, with a Ki of 7.066 μM against human TNF, an IC50 of 9 μM against human COX-2, and an IC50 of 5 μM against ovine COX-1. Roburic acid reduces the production of inflammatory mediators such as NO and IL-6 in macrophages by inhibiting the NF-κB and MAPK (p38/JNK) pathways. By competitively inhibiting the TNF-TNF-R1 interaction, Roburic acid blocks the downstream NF-κB signaling pathway, thereby inducing cell cycle arrest and apoptosis in cancer cells. Roburic acid specifically inhibits osteoclastogenesis and bone resorption by suppressing the RANKL/TRAF6/NF-κB/NFATc1 axis. Roburic acid can be used in research related to osteolytic diseases such as osteoporosis, colorectal cancer and inflammatory diseases.
    Roburic acid (Standard)
  • HY-100375R
    Diroximel fumarate (Standard)
    		Activator
    Diroximel fumarate (Standard) is the analytical standard of Diroximel fumarate (HY-100375). This product is intended for research and analytical applications. Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity.
    Diroximel fumarate (Standard)
  • HY-N0787R
    Cryptochlorogenic acid (Standard)
    		Activator
    Cryptochlorogenic acid (Standard) is the analytical standard of Cryptochlorogenic acid. This product is intended for research and analytical applications. Cryptochlorogenic acid is a natural product.
    Cryptochlorogenic acid (Standard)
  • HY-120912R
    Gingerenone A (Standard)
    		Activator
    Gingerenone A (Standard) is the analytical standard of Gingerenone A. This product is intended for research and analytical applications. 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 (Standard)
Cat. No. 상품명 / Synonyms Application Reactivity