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 관련 제품 (544)
관련 제품 (544)
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Antibodies (7)
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OXPHOS-IN-2
0 ImagesCat. No.: HY-176284OXPHOS-IN-2 is an orally active OXPHOS inhibitor. OXPHOS-IN-2 exhibits potent inhibitory activity in PC9 (IC50 = 12.3 nM) and Bxpc-3 cells (IC50 = 250 nM in glucose medium, IC50 = 17.5 nM in galactose medium). OXPHOS-IN-2 decreases the NADH/NAD+ ratio and reduces ATP levels. OXPHOS-IN-2 induces tumor cells apoptosis by activating reactive oxygen species (ROS) and downregulating the level of Nrf2. OXPHOS-IN-2 can be used for research on cancer such as non-small cell lung cancer and pancreatic cancer.
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CX-Se13
0 ImagesCat. No.: HY-187219CX-Se13 is an orally active pulmonary fibrosis inhibitor with anti-inflammatory and antioxidant activities. CX-Se13 regulates the Keap1/Nrf2/HO-1/NQO1, YAP/TAZ-TEAD, NF-κB p65 and TGF-β/Smads signaling pathways. CX-Se13 activates the cellular antioxidant defense system, restores redox balance, alleviates inflammatory responses, reduces collagen deposition, decreases pro-inflammatory cytokine levels and inhibits pathological progression. CX-Se13 can be used in studies related to pulmonary fibrosis.
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TLR4/NF-κB-IN-2
0 ImagesCat. No.: HY-181765TLR4/NF-κB-IN-2 is an orally active TLR4/NF-κB inhibitor and Nrf2/HO-1 activator. TLR4/NF-κB-IN-2 combats oxidative stress and exerts anti-inflammatory effects by regulating the Nrf2/HO-1 and TLR4/NF-κB pathways. TLR4/NF-κB-IN-2 reduces Aβ aggregation and protects neurons. TLR4/NF-κB-IN-2 can be used in the research of Alzheimer's disease.
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S21-1011
0 ImagesCat. No.: HY-161643CAS No.: 2671859-87-1S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model.
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Cephaeline dihydrobromide
0 ImagesSynonyms: (-)-Cephaeline dihydrobromide; NSC 32944 dihydrobromideCephaeline dihydrobromide ((-)-Cephaeline dihydrobromide; NSC 32944 dihydrobromide) is a ferroptosis inducer, with broad-spectrum anticancer and antiviral activities. Cephaeline dihydrobromide induces ferroptosis (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 dihydrobromide inhibits cancer cell proliferation, migration and tumor growth. Cephaeline dihydrobromide 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 dihydrobromide can be used in studies related to breast cancer, lung cancer, COVID-19, EBOV and ZIKV infections.
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P2Y1 antagonist 4
0 ImagesCat. No.: HY-175675CAS No.: 3104888-50-5P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction.
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(E)-Tadehaginoside
0 ImagesCat. No.: HY-N15691ACAS No.: 283176-41-0(E)-Tadehaginoside is the E-isomer of Tadehaginoside (HY-N15691). Tadehaginoside, 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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AChE/Nrf2 modulator 1
0 ImagesCat. No.: HY-152037CAS No.: 2417117-84-9AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease.
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KEAP1-NRF2 PPI-IN-1
0 ImagesCat. No.: HY-170761CAS No.: 3108079-75-7KEAP1-NRF2 PPI-IN-1 (compound 23) is an inhibitor targeting the KEAP1-NRF2 interaction. KEAP1-NRF2 PPI-IN-1 has IC50 values of 136 nM and 62 nM in the DNA damage assays of human TK6 and insect SF9 cell lines, respectively.
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Stigmane B
0 ImagesCat. No.: HY-N10431Stigmane B (Compound 2) is a nuclear factor E2-related factor (Nrf2) activator. Stigmane B downregulates apoptosis and reactive oxygen species (ROS) generation, and increases antioxidant enzyme activities. Stigmane B shows neuroprotective effects.
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MPQPPAK
0 ImagesCat. No.: HY-P12336MPQPPAK is a polypeptide obtained from the enzymatic hydrolysis of C-phycocyanin (HY-D1025) and possesses neuroprotective activity. MPQPPAK enhances the activities of antioxidant enzymes SOD, CAT, and GSH-Px, reduces ROS, inhibits apoptosis and acetylcholinesterase (AChE) activity in brain tissue, and decreases protein carbonyl content. In the MPTP (HY-W114750)-induced zebrafish Parkinson's disease model, MPQPPAK exhibits antioxidant effects, inhibits autophagy and apoptosis, reverses the loss of dopaminergic neurons and cerebral blood vessels, and alleviates motor deficits. MPQPPAK can be used for research on Parkinson's disease.
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Nrf2 activator-27
0 ImagesCat. No.: HY-184690Nrf2 activator-27 is a Nrf2 activator with anti-inflammatory activity. Nrf2 activator-27 increases the expression level of Nrf2, promotes its nuclear translocation, and upregulates the downstream target proteins HO-1 and NQO1. Nrf2 activator-27 reduces the production of NO, TNF-α, IL-1β and IL-6 in LPS-stimulated macrophages. Nrf2 activator-27 can be used for the research of inflammation-related diseases.
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(-)-(E)-Guggulsterone (Standard)
0 ImagesSynonyms: (E)-Guggulsterone (Standard)(-)-(E) -guggulsterone (Standard) is the analytical standard for (-)-(E) -guggulsterone ((E)-Guggulsterone) (HY-N7781). (-)-(E)-Guggulsterone is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
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Keap1-Nrf2-IN-6
0 ImagesCat. No.: HY-143893CAS No.: 3037016-67-1Keap1-Nrf2-IN-6 (compound 64) is a potent and selective Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 41 nM, Kd of 68 nM.
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Loganin (Standard)
0 ImagesSynonyms: Loganoside (Standard)Loganin (Standard) is the analytical standard of Loganin. This product is intended for research and analytical applications. Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI).
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Ginnalin A
0 ImagesCat. No.: HY-N17603CAS No.: 76746-56-0Synonyms: AcertanninGinnalin A (Acertannin) is a Nrf2 activator. Ginnalin A shows antiproliferative activity against HCT116, SW480 and SW620 cells with IC50 values of 24.8, 22.0, and 39.7 μM, respectively. Ginnalin A can induce cancer cells S phase arrest. Ginnalin A can activate the p62-Keap1-Nrf2 signaling pathway, significantly upregulate the mRNA and protein expression of Nrf2, HO-1, and NQO1, and promote the transport of Nrf2 from the cytoplasm to the nucleus. Ginnalin A can be used for the research of colon cancer.
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Nrf2 activator-20
0 ImagesCat. No.: HY-175217CAS No.: 89883-16-9Nrf2 activator-20 is a potent Nrf2 activator with anti-inflammatory and antioxidant activities. Nrf2 activator-20 activates the anti-inflammatory pathway by interfering with the Keap1-Nrf2 interaction and is beneficial in vivo. Nrf2 activator-20 can be used for the study of acute respiratory distress syndrome (ARDS) and ischemia-reperfusion injury.
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CD-10
0 ImagesCat. No.: HY-174395CD-10 is an orally active and BBB-penatrable Keap1-Nrf2 protein-protein interaction (PPI) inhibitor. CD-10 binds to Keap1 with a KD value of 193 nM. CD-10 exhibits potent anti-oxidative and anti-inflammatory effects through Keap1-Nrf2 pathway activation, evidenced by reduced levels of MDA, IL-4, IL-10 and increased expression of HO-1. CD-10 effectively alleviated anxiety and depressive behaviors and restored serum neurotransmitter levels by promoting Nrf2 nuclear translocation in the chronic unpredictable mild stress (CUMS) mouse model. CD-10 can be used for the study of depression.
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Keap1-Nrf2-IN-11
0 ImagesCat. No.: HY-147924CAS No.: 2796292-75-4Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research.
