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 Produits associés (550)
Produits associés (550)
-
Anticorps (7)
-
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.
-
MAAAHR
0 ImagesCat. No.: HY-P12279MAAAHR is a neuroprotective agent. MAAAHR is isolated and purified from C-phycocyanin of Spirulina platensis. MAAAHR induces antioxidant gene expression through activating the Nrf2 signaling pathway. MAAAHR inhibits excessive Autophagy by reducing the expression of proteins such as α-Syn and Parkin. MAAAHR inhibits Apoptosis. MAAAHR scavenges excessive ROS, enhances SOD, CAT, and GSH-Px activities, and reduces protein carbonyl content. MAAAHR inhibits Acetylcholinesterase. MAAAHR protects zebrafish against MPTP (HY-15608)-induced dopaminergic neuronal and neurovascular loss and alleviates motor impairment. MAAAHR can be used for research on Parkinson's disease.
-
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.
-
Nrf2/HO-1 activator 1
0 ImagesCat. No.: HY-151430Nrf2/HO-1 activator 1 (Compound 24) is a potent Nrf2/HO-1 activator, neuroprotective agent. Nrf2/HO-1 activator 1 shows neuroprotective and antioxidant activities. Nrf2/HO-1 activator 1 can be used in Parkinson's disease (PD) research.
-
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.
-
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.
-
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.
-
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.
-
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.
-
Phoxim-d5 (phenyl-d5) (mixture of isomers)
0 ImagesCat. No.: HY-W758414Phoxim-d5 (phenyl-d5) (mixture of isomers) is the deuterated-labeled Phoxim (HY-B0819). Phoxim is an organophosphorus pesticide and an orally active inhibitor of cholinesterase and CYP3A, which induces neurotoxicity in Caenorhabditis elegans and causes nephrotoxicity characterized by glomerular atrophy and interstitial fibrosis. Phoxim induces inhibition of the autophagy pathway. Phoxim induces dopaminergic neuron degeneration and exacerbates Aβ-induced paralysis. Phoxim damages enterocytes and disrupts intestinal barrier integrity. Phoxim induces ROS accumulation. Phoxim induces mitochondrial apoptosis, involving upregulation of Bad, Bax, caspase-3, and caspase-9 and downregulation of Bcl-2. Phoxim inhibits mitochondrial functional enzymes (COX, Ca2+-Mg2+-ATPase, SDH). Phoxim upregulates Nrf2 mRNA expression in the jejunal mucosa. Phoxim increases TNF-α and decreases IL-6 and IL-8 in the intestinal mucosa. Phoxim alters gut microbial composition by increasing total bacteria and Escherichia coli and reducing Lactobacillus. Phoxim enhances energy metabolism in silver carp by upregulating key glycolytic and gluconeogenic enzymes. Phoxim is used in research on neurodegenerative diseases, nephrotoxicity, intestinal oxidative stress and barrier dysfunction, and bacterial sepsis.
-
GSK3227634
0 ImagesCat. No.: HY-189367CAS No.: 1799977-30-2GSK3227634 is a non-covalent inhibitor of the KEAP1-NRF2 protein-protein interaction. GSK3227634 binds to the Kelch domain of KEAP1, disrupts the KEAP1-NRF2 protein-protein interaction, and thereby activates the NRF2 antioxidant cytoprotective pathway. In a rat model of acute lung injury, intratracheal administration of GSK3227634 dose-dependently upregulates the expression of NRF2 downstream target genes such as NQO1, TXNRD1, and SRXN1, and elevates glutathione levels in lung tissue. GSK3227634 can be used for research on chronic obstructive pulmonary disease.
-
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.
-
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.
-
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.
-
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.
-
VO-OHPic
0 ImagesCat. No.: HY-110067CAS No.: 675848-25-6VO-OHPic is a reversible, noncompetitive PTEN inhibitor with an human IC50 value of 46 nM. VO-OHPic inhibits PTEN signaling, activates Akt-GSK3β and Nrf-2/HO-1 pathways, induces apoptosis resistance and elevates IL-10 levels. VO-OHPic inhibits autophagy, ferroptosis and oxidative stress. VO-OHPic can be used for the research of acute myocardial infarction, intervertebral disc degeneration, cardiomyopathy and cancer.
-
Gymnoside II
0 ImagesCat. No.: HY-N16929CAS No.: 899430-02-5Gymnoside II is one of the main bioactive constituents isolated from Bletilla striata. Gymnoside II inhibits nano SiO2-induced A549 cell viability reduction, apoptosis, and ROS generation by activating Nrf2. Gymnoside II upregulates HO-1 and γ-GCSc, while downregulating the Bax/Bcl-2 ratio. Gymnoside II is applicable for research on nano SiO2-induced pulmonary injury.
-
Dyclonine
0 ImagesDyclonine (Dyclocaine) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis.
-
VH9
0 ImagesCat. No.: HY-P11916VH9 is a Free radical scavenger. VH9 binds to the active pocket of Keap1, blocks the interaction between Keap1 and Nrf2, and activates the Keap1-Nrf2 antioxidant pathway. VH9 inhibits ROS production. VH9 scavenges ABTS and DPPH free radicals through hydrogen bonding and hydrophobic interactions. VH9 protects cells from oxidative stress damage.
