- 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 (525)
Related Products (525)
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Antibodies (7)
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Danshensu
0 ImagesSynonyms: Dan shen suan A; Salvianic acid ADanshensu (Dan shen suan A), an orally active phenolic compound, can induce Nrf2/HO-1 activation and inhibition of NF-κB pathway. Danshensu reduces reactive oxygen species (ROS) production, upregulates antioxidant defense mechanism and inhibits intrinsic apoptotic pathway. Danshensu displays a potent antiviral activity against SARS-CoV-2 with EC50 of 0.97 μM. Danshensu has anti-oxidation, anti-apoptosis, anti-lung inflammatory and has the potential for COVID-19, cardiovascular and cerebrovascular diseases research. -
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VVD-130037
0 ImagesSynonyms: BAY-3605349VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors. -
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Gingerenone A
0 ImagesGingerenone 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. -
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Madecassoside
0 ImagesSynonyms: Asiaticoside AMadecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases. -
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4-Hydroxyphenylacetic acid
0 Images4-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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ML334
0 ImagesSynonyms: LH601AML334 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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CBR-470-1
0 ImagesCBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP+-induced cytotoxicity through activation of the Keap1-Nrf2 cascade. -
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- CDDO-Im
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Cryptochlorogenic acid
0 ImagesSynonyms: 4-Caffeoylquinic acid; 4-O-Caffeoylquinic acidCryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response. -
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Lentinan
0 ImagesCat. No.: HY-N6653CAS No.: 37339-90-5Lentinan is an orally active biocompatible multifunctional polysaccharide with biological activities such as anti-inflammatory, antioxidant, immune regulation, anti-tumor, hypoglycemic, and lipid-lowering[1][4]. -
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Oltipraz
0 ImagesSynonyms: RP 35972; NSC 347901 -
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- Astilbin
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Lithospermic acid
0 ImagesSynonyms: (+)-Lithospermic acidLithospermic 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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Resveratrol (Standard)
0 ImagesSynonyms: trans-Resveratrol (Standard); SRT501 (Standard)Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. 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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Rutaecarpine
0 ImagesRutaecarpine, 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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Curcumin (Standard)
0 ImagesSynonyms: Diferuloylmethane (Standard); Natural Yellow 3 (Standard); Turmeric yellow (Standard)Curcumin (Standard) is the analytical standard of Curcumin (HY-N0005). This product is intended for research and analytical applications. 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. -
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L-Cystine dihydrochloride
0 ImagesL-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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3-Hydroxyphenylacetic acid
0 Images3-Hydroxyphenylacetic acid is an orally active flavonoid metabolite produced by intestinal flora, with blood pressure-lowering activity. 3-Hydroxyphenylacetic acid can also inhibit ferroptosis by upregulating the expression of GPX4, thereby improving spermatogenic dysfunction in aged mice. In addition, abnormal levels of 3-Hydroxyphenylacetic acid are closely related to certain diseases, such as autism spectrum disorders. -
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Sappanone A
0 ImagesSappanone A is an orally active homoisoflavone found in sappan L. Sappanone A is a PDE4 and NF-κB inhibitor with anti-inflammatory and antioxidant effect. Sappanone A induces HO-1 expression through activation of Nrf2 pathway. Sappanone A also inhibits RANKL-induced osteoclastogenesis. Sappanone A has great potential in the research of inflammation-related and cardiovascular . -
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Dendrobine
0 ImagesDendrobine is an alkaloid isolated from Dendrobium nobile. Dendrobine possesses antiviral activity against influenza A viruses, with IC50s of 3.39 μM, 2.16 μM and 5.32 μM for A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2), respectively. Dendrobine activates the JNK/p38/Nrf2 signaling pathway. Dendrobine exhibits antiviral, antitumor, anti-inflammatory, and neuroprotective properties. -
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