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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Anticonvulsant agent 10
0 ImagesCat. No.: HY-173181Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a potent ED50 of 0.04 mmol/kg. By inhibiting Keap1-Nrf2 binding and activating the Nrf2/ARE pathway, Anticonvulsant agent 10 exerts anticonvulsant and neuroprotective effects, making it suitable for research in antiepileptic and neuroprotective studies.
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Nrf2/HO-1 activator 3
0 ImagesCat. No.: HY-170867Nrf2/HO-1 activator 3 (Compound C3a) is the activator for Nrf2 signaling pathway that promotes the Nrf2 translocation into nuclei and upregulates the expression of heme oxygenase-1 HO-1. Nrf2/HO-1 activator 3 inhibits the overespression of ROS and MDA in H2O2- or glucose-stimulated H9c2 cardiomyocytes, inhibits the cell viability and colony formation, thereby exhibiting antioxidant efficacy.
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Alginate oligosaccharides
0 ImagesCat. No.: HY-N20693Synonyms: AOSAlginate oligosaccharides (AOS) are orally effective linear oligosaccharides with anti-inflammatory, antioxidant and antimicrobial activities. Alginate oligosaccharides inhibit the activation of NLRP3 inflammasome and NF-κB, promote nuclear translocation of Nrf2 and phosphorylation of AMPK, and reduce the enhanced functional level of TRPV1. Alginate oligosaccharides improve oxidative stress, ROS production, mitochondrial bioenergetic dysfunction and gait impairment. Alginate oligosaccharides inhibit the release of neuropeptides; alter the structure and viscoelasticity of mucin matrix; disrupt bacterial and fungal biofilms; regulate gut microbiota; and exert anti-apoptotic effects.
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NBE5
0 ImagesCat. No.: HY-181907NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C).
NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
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Nrf-2/HMOX-1-IN-1
0 ImagesCat. No.: HY-184288Nrf-2/HMOX-1-IN-1 is a Nrf-2 and HMOX-1 inhibitor, as well as a Ferroptosis inducer. Nrf-2/HMOX-1-IN-1 inhibits GPX activity and upregulates p53 gene expression. Nrf-2/HMOX-1-IN-1 increases intracellular ROS and MDA levels, reduces GSH content, and elevates intracellular iron levels simultaneously. Nrf-2/HMOX-1-IN-1 exerts selective anticancer effects against breast cancer. Nrf-2/HMOX-1-IN-1 can be used in breast cancer-related research.
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Carlinoside
0 ImagesCat. No.: HY-125129CAS No.: 59952-97-5Carlinoside 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.
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Pyridoxine (Standard)
0 ImagesPyridoxine (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.
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Tovophyllin A
0 ImagesCat. No.: HY-N18091CAS No.: 40738-44-1Tovophyllin A is an orally active xanthonoid compound. Tovophyllin A exerts neuroprotective effects against Parkinson's disease by activating the Akt/GSK3β signaling pathway. Tovophyllin A protects mouse models of liver injury by activating Nrf2. Tovophyllin A exhibits protective anti-inflammatory activity in mouse models of acute lung injury. Tovophyllin A inhibits the activation of NF-κB and subsequent release of pro-inflammatory cytokines. Tovophyllin A reduces apoptotic cell death (Apoptosis). Tovophyllin A has antiplasmodial activity. Tovophyllin A shows cytotoxic activity against lung epithelial cancer cells and breast cancer cells. Tovophyllin A can be used in research related to Parkinson's disease, liver injury, acute lung injury, lung epithelial cancer, and breast cancer.
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FSVVPSPK
0 ImagesCat. No.: HY-P11608CAS No.: 2016043-82-4FSVVPSPK is an orally active peptide. FSVVPSPK exerts significant anti-adipogenic, antioxidant and anti-inflammatory effects in vitro and in vivo, mainly through activating the HO-1/Nrf2 pathway. FSVVPSPK can be used in research related to obesity and metabolic disorders.
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JHB-17
0 ImagesCat. No.: HY-184115JHB-17 is an IKKβ inhibitor with blood-brain barrier permeability, with an IC50 of 1.1 μM and a KD of 1.293 μM. JHB-17 is a non-ATP competitive inhibitor targeting the allosteric site of IKKβ, and it inhibits the phosphorylation of IKKβ. JHB-17 promotes the nuclear translocation of Nrf2, upregulates the expression of HO-1, SLC7A11 and glutathione, and reduces ROS to exert antioxidant effects. JHB-17 reduces cerebral infarction volume and improves neurobehavioral function. JHB-17 can be used in the research of cerebral ischemia-reperfusion injury.
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SH543
0 ImagesCat. No.: HY-180112SH543 is a potent anti-osteoporosis agent. SH543 inhibits nuclear factor κB ligand (RANKL)-induced osteoclastogenesis with an IC50 of 3.3 nM. SH543 directly binds to KEAP1, activates the Nrf2-HO-1 antioxidant pathway, reduces ROS levels, and inhibits PI3K-AKT and MAPK signaling pathways. SH543 attenuates pathological bone loss in ovariectomized mice. SH543 can be used for osteoporosis research.
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4-Hydroxyphenylacetic acid-d2
0 ImagesCat. No.: HY-N1902S24-Hydroxyphenylacetic acid-d2 is the deuterium labeled 4-Hydroxyphenylacetic acid (HY-N1902). 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2.
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TBE 31
0 ImagesCat. No.: HY-141439CAS No.: 936475-62-6TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis.
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Ferroptosis-IN-24
0 ImagesCat. No.: HY-182390Ferroptosis-IN-24 is a non-classical ferroptosis inhibitor capable of crossing the blood-brain barrier, with nanomolar inhibitory activity against ferroptosis induced by RSL3 (HY-100218A) and Erastin (HY-15763). Ferroptosis-IN-24 alleviates oxidative stress, reduces lipid peroxidation accumulation, and restores redox homeostasis. Ferroptosis-IN-24 is applicable to research related to cerebral ischemia-reperfusion injury and acute liver injury.
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Isoeucommin A
0 ImagesCat. No.: HY-N19615CAS No.: 134859-90-8Isoeucommin A is a lignan compound. Isoeucommin A activates the Nrf2/HO-1 pathway and induces phosphorylation of GSK-3β. Isoeucommin A reduces the levels of pro-inflammatory cytokines TNF-α, IL-1β and IL-6, decreases the oxidative stress marker MDA, increases the antioxidants SOD and GSH, and alleviates oxidative stress in mesangial cells. Isoeucommin A alleviates renal tissue injury, improves impaired renal function and enhances the viability of renal tubular epithelial cells in diabetic nephropathy models. Isoeucommin A can be used in the research of diabetic nephropathy.
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Propoxur (Standard)
0 ImagesPropoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.
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Nrf2 activator 18
0 ImagesCat. No.: HY-168709Nrf2 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.
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7-Deacetylgedunin
0 ImagesCat. No.: HY-124941CAS No.: 10314-90-67-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.
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(Rac)-Salvianic acid A sodium (Standard)
0 ImagesCat. No.: HY-N0106RCAS No.: 67920-52-9Synonyms: (Rac)-Danshensu sodium (Standard); (Rac)-Tanshinol sodium (Standard)(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.
