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 (530)
Related Products (530)
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Antibodies (7)
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Dehydrobruceine B
0 ImagesCat. No.: HY-N10313CAS No.: 53730-90-8Dehydrobruceine B, a quassinoid, can be isolated from Brucea javanica. Dehydrobruceine B shows a synergistic effect with Cisplatin (HY-17394) to induce apoptosis via mitochondrial method. Dehydrobruceine B increases apoptosis-inducing factor (AIF) and Bax expression and suppresses Keap1-Nrf2.
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2-Trifluoromethyl-2'-methoxychalcone
0 ImagesCat. No.: HY-124345CAS No.: 1309371-03-62-Trifluoromethyl-2'-methoxychalcone is a chalcone derivative. 2-Trifluoromethyl-2'-methoxychalcone is a potent Nrf2 activator. 2-Trifluoromethyl-2'-methoxychalcone can be used for oxidative stress and inflammation related diseases research.
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Keap1-Nrf2-IN-15
0 ImagesCat. No.: HY-149245CAS No.: 2456295-45-5Keap1-Nrf2-IN-15 (Compound 24a) is a potent Keap1-Nrf2 protein-protein interaction inhibitor with IC50s of 77 nM and 2.5 nM in FP assay and TR-FRET assay, respectively.
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Keap1-Nrf2-IN-12
0 ImagesCat. No.: HY-150578CAS No.: 2250082-04-1Keap1-Nrf2-IN-12 is a potent Keap1-Nrf2 inhibitor with an IC50 value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes.
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Toralactone (Standard)
0 ImagesCat. No.: HY-N7617RCAS No.: 41743-74-2Pirimiphos ethyl (Standard) is the analytical standard of Pirimiphos ethyl. This product is intended for research and analytical applications. Pirimiphos ethyl is a kind of organophosphorus pesticide that commonly employes for the protection of crops including vegetables, bananas, turf and mushrooms through the inhibition of acetylcholinesterase activity.
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3-Hydroxyphenylacetic acid (Standard)
0 Images3-Hydroxyphenylacetic acid (Standard) is the analytical standard of 3-Hydroxyphenylacetic acid (HY-W001083). This product is intended for research and analytical applications. 3-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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LM-1554
0 ImagesCat. No.: HY-W349716CAS No.: 89567-03-3LM-1554 is an orally active antihyperlipaemic agent. LM-1554 can inhibit cholesterol absorption in the gastrointestinal tract.
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4-Octyl itaconate (Standard)
0 ImagesSynonyms: 4-OI (Standard)4-Octyl itaconate (Standard) is the analytical standard of 4-Octyl itaconate. This product is intended for research and analytical applications. 4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1[1].
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α-Tubulin polymerization-IN-1
0 ImagesCat. No.: HY-173039α-Tubulin polymerization-IN-1 (Compound 8l) is an inhibitor for α-Tubulin polymerization. α-Tubulin polymerization-IN-1 modulates the NRF2/KEAP-1 signaling pathway, induces ROS generation in PC-3 cell, thereby inducing apoptosis in PC-3. α-Tubulin polymerization-IN-1 inhibits the proliferation of PC-3 cell with a GI50 of 0.17 µM, arrests the cell cycle at G2/M phase. α-Tubulin polymerization-IN-1 exhibits antitumor efficacy in mouse model.
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Selenomethionine-77Se
0 ImagesCat. No.: HY-B1000S1CAS No.: 1414810-73-3Selenomethionine-77Se (Seleno-DL-methionine-77Se) is the 77Se- labeled Selenomethionine (HY-B1000). Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity.
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Resveratrol (GMP)
0 ImagesResveratrol (GMP) is Resveratrol (HY-16561) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. 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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17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid
0 ImagesCat. No.: HY-139408CAS No.: 1233715-28-0Synonyms: 17-Oxo-DHA; 17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-DHA17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid (17-Oxo-DHA) is a metabolite of lipoxygenase-mediated oxidation of DHA. 17-Oxo-4(Z),7(Z),10(Z),13(Z),15(E),19(Z)-docosahexaenoic acid is a PPARγ agonist and activates a Nrf2 dependent antioxidant reaction.
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NEPP11
0 ImagesCat. No.: HY-180327CAS No.: 313051-12-6NEPP11 is a cyclopentenone prostaglandin analogue. NEPP11 can inhibit glutamate-induced HT22 cell death in mouse hippocampus and prevent manganese-induced apoptosis in PC12 cells. NEPP11 can activate Nrf2 and maintain MEK1/2 and ERK1/2 activity by inhibiting c-Raf downregulation. NEPP11 exerts a neuroprotective effect in a mouse model of focal cerebral ischemia caused by permanent middle cerebral artery occlusion.
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PIISVYWK
0 ImagesCat. No.: HY-P11589CAS No.: 2016043-80-2
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DC-PGKI
0 ImagesCat. No.: HY-177944CAS No.: 2829198-49-2DC-PGKI is an orally active ATP-competitive PGK1 inhibitor(IC50 = 0.16 Μm, Kd = 99.08 nM). DC-PGKI stabilizes PGK1 in vitro and in vivo, and suppresses both glycolytic activity and the kinase function of PGK1. DC-PGKI-mediated inhibition of PGK1 leads to the accumulation of NRF2 (nuclear factor-erythroid factor 2-related factor 2, NFE2L2), which then translocates to the nucleus, binds to the proximal regions of IL-1β and IL-6 genes, and suppresses the LPS-induced expression of these genes. DC-PGKI can be used for the study of colitis.
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Methyl 3,4-dihydroxybenzoate-d3-1
0 ImagesCat. No.: HY-Z0548S1CAS No.: 2733147-54-9Methyl 3,4-dihydroxybenzoate-d3-1 is the deuterium labeled Methyl 3,4-dihydroxybenzoate. 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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Ezetimibe-13C6
0 ImagesCat. No.: HY-17376S3CAS No.: 438624-68-1Synonyms: SCH 58235-13C6
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Bisdemethoxycurcumin
0 ImagesCat. No.: HY-N2942CAS No.: 52328-96-8Bisdemethoxycurcumin is an orally effective curcuminoid. Bisdemethoxycurcumin downregulates pro-inflammatory cytokines in macrophages by inhibiting the phosphorylation of PI3K/Akt and p38 MAPK. Bisdemethoxycurcumin relieves autophagy inhibition and promotes lipophagy to clear vascular smooth muscle foam cells by inhibiting the PDK1/Akt/mTOR pathway. Bisdemethoxycurcumin activates the cAMP/Epac/AMPKα axis and the NRF2/HO-1 antioxidant axis, thereby indirectly inhibiting the phosphorylation of NF-κB p65 and pro-inflammatory outputs such as IL-1β/IL-6/TNF-α, so as to alleviate pulmonary oxidative stress, inflammatory infiltration and pulmonary edema. Bisdemethoxycurcumin blocks NLRP3-mediated pyroptosis and protects cartilage extracellular matrix degradation by activating NRF2/HO-1. Bisdemethoxycurcumin also exerts a synergistic effect with potassium iodide against Candida.
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Keap1-Nrf2-IN-30
0 ImagesCat. No.: HY-184761Keap1-Nrf2-IN-30 is an orally active, blood-brain barrier-permeable Keap1-Nrf2 protein-protein interaction inhibitor with a Keap1 Kd value of 157 nM. Keap1-Nrf2-IN-30 selectively inhibits the Keap1-Nrf2 protein-protein interaction, promotes Nrf2 nuclear translocation, suppresses induced ferroptosis, reduces the expression of Aβ and p-Tau, and upregulates the expression of GPX4 and SLC7A11. Keap1-Nrf2-IN-30 upregulates the expression of HO-1 and NQO1, alleviates neuronal damage, and improves cognitive and spatial memory deficits. Keap1-Nrf2-IN-30 can be used in the research of Alzheimer's disease.
