- Signaling Pathways
- NF-κB
- 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.
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Keap1-Nrf2 Related Products (530)
Related Products (530)
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Antibodies (7)
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Fraxinellone analog 1
0 ImagesCat. No.: HY-163772CAS No.: 3077293-85-4Fraxinellone 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. -
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Dyclonine-d9 hydrochloride
0 ImagesCat. No.: HY-B0364ASSynonyms: Dyclocaine-d9 hydrochlorideDyclonine-d9 hydrochloride (Dyclocaine-d9 hydrochloride) is the deuterated-labeled Dyclonine hydrochloride (HY-B0364A). Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis. -
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4-Octyl itaconate-Bn-S-NH2
0 ImagesCat. No.: HY-1805294-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. -
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HDAC-IN-77
0 ImagesCat. No.: HY-169014HDAC-IN-77 (HL-5s) is an HDAC inhibitor. HDAC-IN-77 can induce ferroptosis and inhibit the Nrf2/HO-1 signaling pathway. HDAC-IN-77 can be used in cancer research. -
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L-Cystine disodium monohydrate
0 ImagesCat. No.: HY-W772717CAS No.: 199329-53-8L-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. -
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Resveratrol-13C6
0 ImagesCat. No.: HY-16561S1Synonyms: trans-Resveratrol-13C6; SRT501-13C6Resveratrol-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. -
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TML-6-d3
0 ImagesCat. No.: HY-137315SCAS No.: 2673270-28-3 -
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AI-3
0 ImagesCat. No.: HY-107736CAS No.: 882288-28-0AI-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. -
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Keap1-Nrf2-IN-5
0 ImagesCat. No.: HY-143892CAS No.: 2696272-70-3Keap1-Nrf2-IN-5 (compound 1) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 4.1 µM, Kd of 3.7 µM. -
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Glycycoumarin (Standard)
0 ImagesCat. No.: HY-N4113RCAS No.: 94805-82-0Glycycoumarin (Standard) is the analytical standard of Glycycoumarin. This product is intended for research and analytical applications. 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. -
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MAGL-IN-22
0 ImagesCat. No.: HY-175270CAS No.: 2720674-71-3MAGL-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. -
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- PROTAC K-Ras Degrader-7
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Nrf2/HO-1 activator 2
0 ImagesCat. No.: HY-151431CAS No.: 2883506-31-6Nrf2/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). -
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Carveol (Standard)
0 ImagesCat. No.: HY-W017370RCAS No.: 99-48-9Carveol (Standard) is the analytical standard of Carveol. This product is intended for research and analytical applications. Carveol is an orally active monoterpenoid alcohol with neuroprotective, antioxidant, anti-inflammatory, anticonvulsant, antidiabetic, hypolipidemic and hepatoprotective activities. Carveol upregulates the expression of Bcl2, downregulates the expression of caspase-3, TNF-α, IL1β and IL6, activates the Nrf2/HO-1 antioxidant signaling pathway, inhibits the RAGE/NF-κB signaling pathway, and suppresses neuroinflammation and neuronal apoptosis. Carveol inhibits α-synuclein aggregation, improves cognitive ability, and inhibits α-amylase activity. Carveol exerts neuroprotective effects in a rat model of Parkinson's disease. Carveol exhibits antidiabetic effects in alloxan-induced diabetic rats. Carveol alleviates PTZ-induced seizures in rats. Carveol can be used in research related to Parkinson's disease, epilepsy, diabetes and ischemic stroke. -
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Tadehaginoside
0 ImagesCat. No.: HY-N15691CAS No.: 2020004-61-7Tadehaginoside, a phenylpropanoid glycoside, is a regulator of lipogenesis and glucose consumption. Tadehaginoside has antioxygenic property. Tadehaginoside mediates liver protection against oxidative stress injury and inflammation by regulating Nrf2 and NF-κB signaling pathways in hepatocytes. Tadehaginoside can be used for the study of obesity and diabetes. -
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Citraconic acid (Standard)
0 ImagesSynonyms: Methylmaleic acid (Standard); Citraconate (Standard)Citraconic acid (Methylmaleic acid) (Standard) is the analytical standard of Citraconic acid (HY-113298). This product is intended for research and analytical applications. Citraconic 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). -
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Nrf2/HO-1 activator 4
0 ImagesCat. No.: HY-184698CAS No.: 3072761-08-8Nrf2/HO-1 activator 4 is a Nrf2/HO-1 activator. Nrf2/HO-1 activator 4 inhibits nitric oxide production and the expression of pro-inflammatory cytokines IL-1β, IL-6, TNF-α, as well as upstream inflammatory enzymes COX-2 and iNOS. Nrf2/HO-1 activator 4 reduces ROS accumulation, and restores GSH levels and SOD activity. Nrf2/HO-1 activator 4 ameliorates depression-like behaviors in mice. Nrf2/HO-1 activator 4 can be used for research on major depressive disorder. -
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Keap1-Nrf2-IN-18
0 ImagesCat. No.: HY-157928Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM). -
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Methyl 3,4-dihydroxybenzoate (Standard)
0 ImagesSynonyms: Protocatechuic acid methyl ester (Standard); Methyl protocatechuate (Standard)Methyl 3,4-dihydroxybenzoate (Standard) is the analytical standard of Methyl 3,4-dihydroxybenzoate. This product is intended for research and analytical applications. 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. -
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AChE-IN-105
0 ImagesCat. No.: HY-180946CAS No.: 2678601-07-3AChE-IN-105 (Compound C5) is a potent, mixed AChE inhibitor with an IC50 of 5.02 μM. AChE-IN-105 scavenges ROS, decreases Hydrogen peroxide-induced Caspase-3 activation, reduces activity of the Nrf2-ARE pathway. AChE-IN-105 prevents memory impairments in the Scopolamine (HY-N0296)-induced cognitive dysfunction zebrafish model. AChE-IN-105 has potent antioxidant activity. AChE-IN-105 can be used in the research of Alzheimer's disease. -
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