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.
All Product Categories
-
Keap1-Nrf2 Related Products (525)
Related Products (525)
-
Antibodies (7)
-
Isorhapontigenin (Standard)
0 ImagesCat. No.: HY-N2593RCAS No.: 32507-66-7Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin (HY-N2593). This product is intended for research and analytical applications. Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
-
Obtusaquinone
0 ImagesCat. No.: HY-N19738CAS No.: 21105-15-7Obtusaquinone is a blood-brain barrier-permeable Keap1 inhibitor with anticancer activity. Obtusaquinone covalently binds to cysteine residues of Keap1, promotes its ubiquitination and proteasomal degradation, and activates the Nrf2 pathway. Obtusaquinone induces endoplasmic reticulum stress and DNA damage through abnormal accumulation of ROS, and triggers apoptosis of cancer cells. Obtusaquinone prolongs survival in orthotopic xenograft models of pediatric high-grade glioma, and exhibits antitumor activity in glioblastoma and breast cancer models. Obtusaquinone can be used in studies related to glioma and breast cancer.
-
Keap1-p-p62-IN-1
0 ImagesCat. No.: HY-184204Keap1-p-p62-IN-1 is a potent and selective Keap1-p-p62 inhibitor with an IC50 of 0.11 μM. Keap1-p-p62-IN-1 shows 18.73-fold selectivity over Keap1-Nrf2 interaction. Keap1-p-p62-IN-1 normalizes Nrf2 ubiquitination, sensitizes cells to Sorafenib (HY-10201)-induced ferroptosis. Keap1-p-p62-IN-1 can be used for the research of p62 aberrant hepatocellular carcinoma.
-
Keap1-Nrf2-IN-22
0 ImagesCat. No.: HY-168065CAS No.: 2955083-85-7Keap1-Nrf2-IN-22 (compound 19) is a Keap1-Nrf2 inhibitor， with a KD2 value of 42.2 nM for Keap1. Keap1-Nrf2-IN-22 can be used for the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury.
-
Selenomethionine-76Se
0 ImagesCat. No.: HY-B1000SCAS No.: 2108158-10-5Synonyms: Seleno-DL-methionine-76Se; DL-Selenomethionine-76SeSelenomethionine-76Se (Seleno-DL-methionine-76Se) is the 76Se- 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.
-
Propoxur-d7
0 ImagesCat. No.: HY-W750153CAS No.: 2140327-65-5Propoxur-d7 is the deuterium labeled Propoxur. 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.
-
Pulegone-d8
0 ImagesCat. No.: HY-N1500S1CAS No.: 62385-90-4Pulegone-d8 is deuterated labeled Pulegone (HY-N1500). Pulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.
-
Corynoline (Standard)
0 ImagesCat. No.: HY-N0826RCAS No.: 18797-79-0Corynoline (Standard) is the analytical standard of Corynoline. This product is intended for research and analytical applications. Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits anti-inflammatory activity by activating Nrf2.
-
Keap1-Nrf2-IN-25
0 ImagesCat. No.: HY-168922CAS No.: 3100306-80-4Keap1-Nrf2-IN-25 (Compound 19) is a potent Keap1-Nrf2 inhibitor (IC50 of 0.55 μM) with Keap1 binding affinity (Kd of 0.50 μM). Keap1-Nrf2-IN-25 activates Nrf2, reduces ROS and pro-inflammatory cytokines (IL-1β, IL-6). Keap1-Nrf2-IN-25 exerts protective effects against DSS (HY-116282)-induced colitis.
-
4-Methoxychalcone-1
0 Images4-Methoxychalcone is a naturally occurring chalcone compound. 4-Methoxychalcone has antioxidant activity, anti-inflammatory activity, antitumor activity and antibacterial activity. 4-Methoxychalcone can be used to study inflammation and tumor models.
-
3-Hydroxyphenylacetic acid-d6
0 ImagesCat. No.: HY-W001083S23-Hydroxyphenylacetic acid-d6 is the deuterium labeled 3-Hydroxyphenylacetic acid (HY-W001083). 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.
-
Anti-inflammatory agent 72
0 ImagesCat. No.: HY-162170CAS No.: 3036299-85-8Anti-inflammatory agent 72 (compound 5) is a novel resveratrol derivative hybrid with benzoylhydrazine. Anti-inflammatory agent 72 shows anti-inflammatory and antioxidant activities by activating Nrf2 and inhibiting NF-κB p65/iNOS and MAPKs signaling pathways.
-
Anticancer agent 359
0 ImagesCat. No.: HY-187687CAS No.: 2740603-37-4Anticancer agent 359 is a ferroptosis inducer. Anticancer agent 359 inhibits the proliferation, colony formation and migration of bladder cancer cells in a concentration-dependent manner. Anticancer agent 359 induces ferroptosis by downregulating SREBP1 to inhibit FASN transcription, reducing the expression of NRF2/SLC7A11/GPX4, decreasing GSH, promoting ROS accumulation and lipid peroxidation; this effect is reversible by Ferrostatin-1 (HY-100579). Anticancer agent 359 acts synergistically with Talazoparib (HY-16106). Anticancer agent 359 inhibits tumor growth in vivo without obvious hepatotoxicity or nephrotoxicity. Anticancer agent 359 can be used in the research of bladder cancer.
-
Sesaminol
0 ImagesCat. No.: HY-N15190CAS No.: 74061-79-3Sesaminol is an orally active activator for Nrf2-ARE pathway, that promotes the the nuclear translocation of Nrf2 and enhances the NQO1 expression, thereby enhances the cell's defense against oxidative stress. Sesaminol inhibits 6-OHDA (HY-B1081)-induced ROS production and apoptosis in cell SH-SY5Y. Sesaminol exhibits neuroprotective efficacy against Rotenone (HY-B1756)-induced Parkinson's disease.
-
DI-1548
0 ImagesCat. No.: HY-156240CAS No.: 2247060-97-3DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research.
-
Keap1-Nrf2-IN-21
0 ImagesCat. No.: HY-159495Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the Keap1-Nrf2 signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC50=2.60 μM).
-
Dibenzoylmethane (Standard)
0 ImagesCat. No.: HY-W009731RCAS No.: 120-46-7Dibenzoylmethane (Standard) is the analytical standard of Dibenzoylmethane. This product is intended for research and analytical applications. Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2.
-
Nrf2 activator-21
0 ImagesCat. No.: HY-175548CAS No.: 1912404-14-8Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury.
-
Keap1-Nrf2-IN-24
0 ImagesCat. No.: HY-168526Keap1-Nrf2-IN-24 (compound 57) is a potent Keap1-Nrf2 inhibitor with a Ki value of 13 nM. Keap1-Nrf2-IN-24 increases the protein expression of TRXR1 and NQO1. Keap1-Nrf2-IN-24 increases the AKR1B10 mRNA expression. Keap1-Nrf2-IN-24 shows good metabolic stability.
-
Antioxidant agent-5
0 ImagesCat. No.: HY-143243CAS No.: 2684291-60-7Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway.
