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 (525)
Related Products (525)
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Antibodies (7)
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NF-κB-IN-20
0 ImagesCat. No.: HY-175833NF-κB-IN-20 is an orally active NF-κB inhibitor. NF-κB-IN-20 directly binds to the Keap1 protein, activating the Keap1/Nrf2/HO-1 antioxidant pathway, and simultaneously inhibiting the NF-κB inflammatory pathway, thereby synergistically reducing oxidative stress and inflammatory responses. NF-κB-IN-20 M11 inhibits the expression of IL-6, IL-1β, and TNF-α, significantly reduces the level of ROS, and restores the mitochondrial membrane potential. NF-κB-IN-20 can be used for the study of acute lung injury (ALI).
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CF-Vanillin
0 ImagesCat. No.: HY-181474CAS No.: 1323378-95-5CF-Vanillin is an orally active hypolipidemic/hepatic protector with strong binding affinity for PPAR-α. CF-Vanillin exerts antioxidant and anti-inflammatory effects by activating the Nrf2/HO-1 signaling pathway. CF-Vanillin reduces triglyceride and total cholesterol levels and alleviates liver injury. CF-Vanillin can be used in the research of diseases such as hyperlipidemia and liver injury.
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5,7-Dihydroxychromone (Standard)
0 ImagesCat. No.: HY-N1970RCAS No.: 31721-94-55,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone (HY-N1970). This product is intended for research and analytical applications. 5,7-Dihydroxychromone is a flavonoid compound with antioxidant properties. 5,7-Dihydroxychromone induces Nrf2 nuclear translocation, increases Nrf2/ARE binding activity, and up-regulates Nrf2-dependent antioxidant genes HO-1, NQO1, GCLc. 5,7-Dihydroxychromone attenuates excessive ROS generation, inhibits activated caspase-3, caspase-9, cleaved PARP expression, and prevents neuronal apoptosis and cell death. 5,7-Dihydroxychromone increases LXRα and PPARγ mRNA expression, induces preadipocyte differentiation, and regulates blood glucose levels. 5,7-Dihydroxychromone inhibits radial growth of soil pathogenic fungi, radicle elongation of select seedlings, and transiently inhibits Bradyrhizobium sp. growth in high mannitol medium. 5,7-Dihydroxychromone can be used for the research of Parkinson’s disease, type 2 diabetes mellitus and pathogenic fungal infection.
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Keap1-IN-2
0 ImagesCat. No.: HY-174287CAS No.: 3066895-41-5Keap1-IN-2 (Compound 164) is a KEAP1 inhibitor (IC50: 2 nM). Keap1-IN-2 indirectly activates Nrf2 by inhibiting KEAP1, thereby enhancing the antioxidant capacity of cells. Keap1-IN-2 promotes the accumulation and nuclear translocation of Nrf2 by blocking KEAP1-mediated Nrf2 degradation. Keap1-IN-2 can be used to study diseases associated with oxidative stress, such as inflammatory bowel disease, Crohn's disease, and immune diseases such as ulcerative colitis.
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Mycosporine 2 glycine
0 ImagesCat. No.: HY-161612CAS No.: 149092-45-5Mycosporine 2 glycine is an anti-inflammatory agent and TYRP1 inhibitor. Mycosporine 2 glycine inhibits the expression of inflammatory genes and reduces nitric oxide production. Mycosporine 2 glycine binds tightly to the active pocket of TYRP1 and inhibits the activity of melanogenesis-related enzymes. Mycosporine 2 glycine can be used in the research of hyperpigmentation and inflammation-related diseases.
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L-Cystine dihydrochloride (Standard)
0 ImagesCat. No.: HY-W009203RCAS No.: 30925-07-6L-Cystine (dihydrochloride) (Standard) is the analytical standard of L-Cystine (dihydrochloride) (HY-W009203). This product is intended for research and analytical applications. 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
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Dyclonine hydrochloride (Standard)
0 ImagesSynonyms: Dyclocaine hydrochloride (Standard)Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. 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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Pyridoxine-d2
0 ImagesCat. No.: HY-B1328S2CAS No.: 5027-84-9Synonyms: Pyridoxol-d2Pyridoxine-d2 (Pyridoxol-d2) is deuterium labeled Pyridoxine. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
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NFE2L2 activator 3
0 ImagesCat. No.: HY-125995CAS No.: 2230581-03-8NFE2L2 activator 3 (Compound 3) is a NFE2L2/NRF2 activator. NFE2L2 activator 3 specifically activates the NAD(P)H:quinone oxidoreductase (NQO1) enzyme, with its EC50 < 1 nM. NFE2L2 activator 3 can be used for research on respiratory system diseases such as chronic obstructive pulmonary disease.
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Monotropein (Standard)
0 ImagesMonotropein (Standard) is the analytical standard of Monotropein. This product is intended for research and analytical applications. Monotropein is an iridoid glycoside that can be isolated from the roots of Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model. Monotropein exerts protective effects against IL-1β-induced apoptosis and catabolic responses on osteoarthritis chondrocytes. Monotropein has cartilage protective activity. Monotropein can alleviate Cisplatin (HY-17394)-induced acute kidney injury by inhibiting oxidative damage, inflammation and apoptosis through activation of Nrf2/HO-1 pathway and inhibition of NF-κB signaling. Monotropein can be studied in research for osteoarthritis, acute kidney injury and acute lung injury.
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TPNA10168
0 ImagesCat. No.: HY-W505984CAS No.: 957942-34-6Synonyms: KM05073TPNA10168 is an Nrf-2 activator that activates the Keap1-Nrf2-ARE pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases.
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Lithospermic acid (Standard)
0 ImagesSynonyms: (+)-Lithospermic acid (Standard)Lithospermic acid (Standard) is the analytical standard of Lithospermic acid. This product is intended for research and analytical applications. 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.
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ML334 (Standard)
0 ImagesCat. No.: HY-110258RCAS No.: 1432500-66-7Synonyms: LH601A (Standard)ML334 (Standard) is the analytical standard of ML334 (HY-110258). This product is intended for research and analytical applications. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
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Necrosulfonamide (Standard)
0 ImagesCat. No.: HY-100573RCAS No.: 1360614-48-7Necrosulfonamide (Standard) is the analytical standard of Necrosulfonamide (HY-100573). This product is intended for research and analytical applications. Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
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WN1316
0 ImagesCat. No.: HY-120570CAS No.: 1356959-71-1WN1316 is an oral active antioxidant agent. WN1316 shows neuroprotectant activity and can be used for study of amyotrophic lateral sclerosis.
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Tanshinlactone
0 ImagesCat. No.: HY-N1180CAS No.: 105351-70-0Tanshinlactone is a compound found in Salvia miltiorrhiza with anti-coronavirus (CoV) and anti-tumor activities. Tanshinlactone induces methuocytic cell death (methuosis) by activating the NRF2 pathway, and selectively kills ER+, HER2+/EGFR+ breast cancer cells. Tanshinlactone is applicable to research related to breast cancer and coronavirus infections.
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CPDT
0 ImagesCat. No.: HY-W975966CAS No.: 14085-33-7CPDT is an orally active and highly potent inducer of phase 2 enzymes and an activator of Nrf2. The activities of key phase 2 enzymes, including glutathione S-transferase, NAD(P)H:quinone:oxidoreductase 1 and glutamate cysteine synthetase, and levels of glutathione were elevated by CPDT in rat bladder in vivo and in cultured bladder cells in vitro[2].
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ALR2-IN-9
0 ImagesCat. No.: HY-175862CAS No.: 2135481-84-2ALR2-IN-9 is a potent ALR2 inhibitor (IC50 = 21.8 nM) with excellent antioxidant activity (EC50 for DPPH radical scavenging = 2.8 μM). ALR2-IN-9 interacts directly with Reactive Oxygen Species (ROS)/Reactive Nitrogen Species (RNS) and interrupts the free radical chain reactions, and as an endogenous enzymatic antioxidant regulator, which regulates enzyme functions of CAT and SOD. ALR2-IN-9 regulates PI3K/Akt/Nrf2 pathway to attenuate hyperglycemia-mediated mitochondrial superoxide overproduction in vitro, and ameliorates CuSO4- and H2O2-induced oxidative stress in vivo. ALR2-IN-9 prolongs lifespan of C. elegans via the regulation of stress response genes such as PMK-1. ALR2-IN-9 is a promising anti-aging drug candidate. ALR2-IN-9 can be used for diabetic complication research.
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KI696 (Standard)
0 ImagesCat. No.: HY-101140RCAS No.: 1799974-70-1KI696 (Standard) is the analytical standard of KI696 (HY-101140). This product is intended for research and analytical applications. KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation.
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Ethyl (E)-ferulate
0 ImagesCat. No.: HY-W590845CAS No.: 28028-62-8Ethyl (E)-ferulate is an AMPK/Nrf2 signaling pathway activator that can reduce lipopolysaccharide (HY-D1056)-induced acute lung injury. Additionally, Ethyl (E)-ferulate exhibits free radical scavenging properties, providing anti-inflammatory, antioxidant, neuroprotective, and sunscreen effects. Ethyl (E)-ferulate holds promise for research in the fields of inflammation and neurodegenerative diseases.
