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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Productos relacionados con Keap1-Nrf2 (549)
Productos relacionados con (549)
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Antibodies (7)
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Keap1-Nrf2-IN-5
0 ImagesReferencia número: HY-143892No. CAS: 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 ImagesReferencia número: HY-N4113RNo. CAS: 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 ImagesReferencia número: HY-175270No. CAS: 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 ImagesReferencia número: HY-151431No. CAS: 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 ImagesReferencia número: HY-W017370RNo. CAS: 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 ImagesReferencia número: HY-N15691No. CAS: 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 ImagesReferencia número: HY-184698No. CAS: 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 ImagesReferencia número: 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 ImagesReferencia número: HY-180946No. CAS: 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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TrxR1-IN-B19
0 ImagesReferencia número: HY-120914No. CAS: 170950-29-5Synonyms: GO-Y015TrxR1-IN-B19 (GO-Y015) is a Curcumin (HY-N0005) derivative and TrxR1 inhibitor. TrxR1-IN-B19 inhibits de novo selenoprotein synthesis, suppresses SeP and GPx expression, and impairs selenium incorporation into Sec-tRNA[Sec]. TrxR1-IN-B19 induces Nrf2 accumulation through Keap1 cysteine modification, HO-1 expression, GSH synthesis, ROS accumulation, ER stress, mitochondrial dysfunction, Apoptosis, and G2/M phase arrest. TrxR1-IN-B19 improves glucose tolerance and insulin sensitivity, lowers blood glucose, inhibits tumor growth, and reduces arsenic accumulation. TrxR1-IN-B19 can be used for research on type 2 diabetes, arsenite-induced toxicity, and gastric cancer.
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Hexadecanedioic acid-d28
0 ImagesHexadecanedioic acid-d28 is the deuterium labeled Hexadecanedioic acid (HY-W018161). Hexadecanedioic acid (Thapsic acid) is an orally active metabolite produced by B. uniformis. Hexadecanedioic acid inhibits IRE1α-XBP1s-mediated flipogenesis and ferroptosis. Hexadecanedioic acid downregulates XBP1 and Hrd1 expression, activates the Nrf2/SLC7A11/GPX4 pathway. Hexadecanedioic acid can be used for the research of metabolic-associated fatty liver disease.
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YPLP
0 ImagesReferencia número: HY-163315No. CAS: 2414391-44-7YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active.
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PRL-295
0 ImagesReferencia número: HY-171035No. CAS: 2377770-85-7PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction. PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice.
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Keap1/Nrf2/ARE activator 2
0 ImagesReferencia número: HY-180155No. CAS: 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 ImagesReferencia número: 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 ImagesReferencia número: 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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Cephaeline hydrochloride
0 ImagesSynonyms: (-)-Cephaeline hydrochloride; NSC 32944 monohydrochlorideCephaeline hydrochloride ((-)-Cephaeline (hydrochloride); NSC 32944 (monohydrochloride)) is a ferroptosis inducer, with broad-spectrum anticancer and antiviral activities. Cephaeline hydrochloride induces Ferroptosis by upregulating p53, inhibiting NRF2, activating ULK3, downregulating the expressions of SLC7A11 and GPX4 in a p53-dependent manner, reducing GSH and mitochondrial membrane potential, and increasing lipid peroxidation and iron accumulation. Cephaeline hydrochloride inhibits cancer cell proliferation, migration and tumor growth. Cephaeline hydrochloride inhibits Ebola virus (EBOV) VLP entry and infection, with IC50 values of 3.27 μM and 22.18 μM respectively; it also inhibits Zika virus (ZIKV) NS5 RdRp activity (IC50 = 976 nM), and binds to severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) RdRp and N protein, with Kd values of 8.9 μM and 53.8 μM respectively. Cephaeline hydrochloride can be used in studies related to breast cancer, lung cancer, COVID-19, EBOV and ZIKV infections.
