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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Propoxur-d3
0 ImagesCat. No.: HY-B0916SCAS No.: 1219798-56-7Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). 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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TBHQ-d12
0 ImagesCat. No.: HY-100489SSynonyms: tert-Butylhydroquinone-d12TBHQ-d12 (tert-Butylhydroquinone-d12) is the deuterium labeled TBHQ (HY-100489). TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma[2].
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Keap1-Nrf2-IN-19
0 ImagesCat. No.: HY-157929Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs.
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SH494
0 ImagesCat. No.: HY-182818SH494 is a p38 MAPK inhibitor and Nrf2 pathway activator. SH494 inhibits RANKL-induced phosphorylation of p38 and disrupts the MAPK cascade associated with osteoclastogenesis. SH494 activates the Nrf2 pathway, upregulates downstream target genes and induces the expression of cytoprotective enzymes. SH494 reduces intracellular ROS accumulation and restores mitochondrial membrane potential (ΔΨm) to normal. SH494 decreases osteoclast activity and alleviates osteoporosis symptoms in ovariectomized mice. SH494 can be used for research on osteoporosis.
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Curdione (Standard)
0 ImagesCat. No.: HY-N0353RCAS No.: 13657-68-6Synonyms: (+)-Curdione (Standard)Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
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SPC-180002
0 ImagesCat. No.: HY-155784CAS No.: 2170274-53-8SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.
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Nrf2 activator-25
0 ImagesCat. No.: HY-183353Nrf2 activator-25 is a Nrf2 activator. Nrf2 activator-25 promotes the dissociation of Nrf2 from Keap1 (with a Kd of 21.3 μM for Keap1), drives Nrf2 nuclear translocation, and increases the production of downstream antioxidant enzymes. Nrf2 activator-25 inhibits apoptosis, ferroptosis and vascular fibrosis, and protects vascular endothelial cells from damage. Nrf2 activator-25 can be used in the research of diabetic vascular diseases.
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Aβ-IN-6
0 ImagesCat. No.: HY-149246CAS No.: 3043752-01-5Aβ-IN-6 reduces pro-inflammatory cytokine release from microglia cells. Aβ-IN-6 significantly induces Nrf2 nuclear translocation and hamperes Aβ oligomers formation. Aβ-IN-6 exerts a consistent neuroprotective effect by modulating the redox-sensitive signalling pathways in vivo oxidative stress model. Aβ-IN-6 is an orally active and has antiinflammatory, Antioxidant and Anti-oligomeric activity. Aβ-IN-6 has the potential for Alzheimer's disease (AD) research.
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NF-κB/HIF-1α-IN-1
0 ImagesCat. No.: HY-173488NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2.
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Keap1-IN-1
0 ImagesCat. No.: HY-170301Keap1-IN-1 (Compound 27) is the inhibitor for Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE)-dependent gene NQO1 with an EC50 of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC50 of 527 nM.
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Keap1-Nrf2-IN-27
0 ImagesCat. No.: HY-173187Keap1-Nrf2-IN-27 (compound 1C) is a inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) with KD2 value of 0.119 μM. Keap1-Nrf2-IN-27 suppresses the expression of pro-inflammatory cytokine TNF-α and IL-6 in the LPS-induced RAW264.7 cell model.
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Anticancer agent 309
0 ImagesCat. No.: HY-182055Anticancer agent 309 (Compound HZ-1) is an anticancer agent and G-quadruplex binder, with Kd values of 2.46 μM and 1.61 μM for c-Myc G4 and KRAS G4, respectively. Anticancer agent 309 promotes the formation of intranuclear G4. Anticancer agent 309 shows higher selectivity for parallel G4 than for non-parallel G4. Anticancer agent 309 inhibits the NRF2 signaling pathway and reduces the expression of XCT and GPX4. Anticancer agent 309 induces Ferroptosis, Apoptosis and immunogenic cell death in cells. Anticancer agent 309 exerts antitumor efficacy against breast cancer. Anticancer agent 309 is applicable for the research of breast cancer.
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Nrf2 activator-23
0 ImagesCat. No.: HY-181887CAS No.: 3109883-60-2Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with KD values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis.
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PACA
0 ImagesCat. No.: HY-116202CAS No.: 1431724-30-9PACA is an enhancer of nerve growth factor-induced neurite outgrowth, enhancing nerve growth factor (NGF)-induced neurite outgrowth and attenuating 6-hydroxydopamine (6-OHDA)-induced toxicity by activating the Nrf2/HO-1 pathway. PACA has neuroprotective and neurogenic activities. PACA can be used to improve dopaminergic neuron loss and motor dysfunction in MPTP mouse models of Parkinson's disease and MPP+-induced neurons.
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Loganic acid (Standard)
0 ImagesCat. No.: HY-N0513RCAS No.: 22255-40-9Loganic acid (Standard) is the analytical standard of Loganic acid. This product is intended for research and analytical applications. Loganic acid is an iridoid isolated from cornelian cherry fruits. Loganic acid inhibits NF-κB signaling pathway, activates Nrf2 signaling pathway, exhibits anti-inflammatory activity. Loganic acid can modulate diet-induced atherosclerosis and redox status. Loganic acid has strong free radical scavenging activity and remarkable cyto-protective effect against heavy metal mediated toxicity. Loganic acid is orally active.
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Esculeogenin A
0 ImagesCat. No.: HY-N18066CAS No.: 854381-37-6Esculeogenin A is the sapogenol of tomato saponin Esculeoside A (HY-N18067). Esculeogenin A is an orally active hepatoprotective, hypolipidemic, and antioxidant agent. Esculeogenin A regulates molecular targets like PPARα, SREBP1, Nrf2, NF-κB, ACAT1/ACAT2 to promote hepatic fatty acid oxidation, suppress de novo lipogenesis, enhance antioxidant defense, and inhibit inflammation. Esculeogenin A improves liver function, alleviates hyperlipidemia, and inhibits hepatic steatosis and foam cell formation, preventing nonalcoholic fatty liver disease in high-fat-diet-fed rats and reducing atherosclerotic lesions in apoE-deficient mice. Esculeogenin A can be used for the research of nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia.
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Azafrin
0 ImagesAzafrin, a carotenoid, is one of the most abundant active ingredients in C. grandiflora. Azafrin increases HO-1, NQO1, and Nrf2 expression. Azafrin shows cardioprotective effect against myocardial injury via activation of the Nrf2-ARE pathway. Azafrin can be used for research of cardiovascular diseases.
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QD 232
0 ImagesCat. No.: HY-120825CAS No.: 1527467-32-8QD 232 is a quinazolinedione-based ROS inducer and an apoptosis inducer with cytotoxicity and redox regulatory activity. QD 232 promotes ROS accumulation, activates the NRF2-mediated oxidative stress response and unfolded protein response pathways, and upregulates downstream antioxidant and stress response genes. QD 232 inhibits mtDNA transcription driven by HSP2 and LSP promoters, and impairs mitochondrial oxidative phosphorylation function. QD 232 induces apoptosis of pancreatic ductal adenocarcinoma cells and exerts cytotoxicity against gemcitabine (HY-17026)-resistant pancreatic ductal adenocarcinoma cells. QD 232 delays tumor growth in a mouse pancreatic cancer xenograft model.
