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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Oltipraz-d3
0 ImagesCat. No.: HY-12519SCAS No.: 2012598-51-3Synonyms: RP 35972-d3; NSC 347901-d3
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FXR agonist 18
0 ImagesCat. No.: HY-183692CAS No.: 3061938-00-6FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.
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Rutaecarpine (Standard)
0 ImagesRutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. 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).
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Pachypodol (Standard)
0 ImagesCat. No.: HY-N3121RCAS No.: 33708-72-4Pachypodol (Standard) is the analytical standard of Pachypodol (HY-N3121). This product is intended for research and analytical applications. Pachypodol is an orally active methoxyflavonoid compound. Pachypodol activates the ERK-dependent Nrf2 pathway and inhibits Apoptosis. Pachypodol exhibits activities such as antioxidant, cytoprotective, anti-inflammatory effects. Pachypodol improves cognition. Pachypodol exerts protective effects against cardiac and liver damage. Pachypodol has anticancer activity against colon cancer.
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Oltipraz (GMP)
0 ImagesCat. No.: HY-12519GCAS No.: 64224-21-1Synonyms: RP 35972 (GMP); NSC 347901 (GMP)
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Clemastine fumarate (Standard)
0 ImagesSynonyms: HS-592 fumarate (Standard); Meclastine fumarate (Standard)Clemastine (HS-592; Meclastine) fumarate (Standard) is the analytical standard of Clemastine fumarate. This product is intended for research and analytical applications. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
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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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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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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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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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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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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/ARE activator 2
0 ImagesCat. No.: HY-180155CAS No.: 3105470-83-2Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease.
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Nrf2 activator-9
0 ImagesCat. No.: HY-156081Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis.
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4,5-Dehydro-6-oxoallosecurinine
0 ImagesCat. No.: HY-1818184,5-Dehydro-6-oxoallosecurinine is a Keap1-Nrf2 pathway activator. 4,5-Dehydro-6-oxoallosecurinine promotes the nuclear translocation of Keap1-Nrf2, and induces the expression of antioxidant and cytoprotective genes. 4,5-Dehydro-6-oxoallosecurinine reduces the production of NO, and decreases the levels of iNOS, TNF-α, IL-6 and IL-1β in LPS-stimulated microglia. 4,5-Dehydro-6-oxoallosecurinine can be used for the research of neurodegenerative diseases.
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MGF24
0 ImagesCat. No.: HY-P11124CAS No.: 1611488-66-4MGF24 is a modified protease-resistant MGF derivative. MGF24 protects dopaminergic neurons from 6-Hydroxydopamine (6-OHDA) (HY-113028)-induced apoptosis by inducing Heme oxygenase-1 (HO-1). MGF24 activates PKC-ε, which in turn activates Nrf2, up-regulating HO-1. MGF24 has neuroprotective activity and reduces myocardial infarct size in sheep models of myocardial ischemia. MGF24 can be used for neurological diseases like stroke, nerve injury and amyotrophic lateral sclerosis research.
