Catalog No.
Product Name
Application
Product Information
Citations
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Neddylation Inhibitor
Keap1-Nrf2-IN-4 is a potent neddylation inhibitor that targets the Keap1-Nrf2 pathway. It exhibits significant anti-proliferative activity against MGC-803 gastric cancer cells, with an IC50 value of 2.55 µM. Additionally, Keap1-Nrf2-IN-4 effectively inhibits cell migration and induces apoptosis in these cancer cells, contributing to tumor growth suppression while exhibiting minimal toxicity. This compound is valuable for research into cancer therapies and the regulation of oxidative stress responses. -
Nrf2 inhibitory protein Keap-1 Activator
KMS99220 is a potent activator of the Nrf2 inhibitory protein Keap-1, capable of crossing the blood-brain barrier. This compound enhances AMPK activity and activates the Nrf2 signaling pathway, leading to decreased phosphorylation of IκB, reduced translocation of NFκB, and modulation of MAPK pathways. KMS99220 promotes the expression of neuroprotective genes, including HO-1 and NQO1, and exhibits anti-inflammatory properties by inhibiting iNOS and IL-1β production. Its application in research focuses on understanding neurodegenerative diseases like Parkinson's disease, particularly its effects on dopaminergic neuron preservation and associated motor dysfunction. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-11 is a potent inhibitor of the Keap1-Nrf2 interaction, exhibiting a KD2 value of 0.21 nM. This compound effectively reduces the production of reactive oxygen species (ROS) and nitric oxide (NO), as well as downregulating the expression of tumor necrosis factor-alpha (TNF-α). By promoting Nrf2 nuclear translocation, Keap1-Nrf2-IN-11 demonstrates significant anti-inflammatory properties, making it a valuable tool for research in inflammation-related pathways. -
Nrf1/Nrf2 Activator
Rosolutamide is a potent Nrf1 and Nrf2 activator that enhances the expression of proteasome subunits, antioxidant enzymes, and molecular chaperones through the activation of these transcription factors. This curcumin analog facilitates the degradation of polyglutamine (polyQ) androgen receptors via the ubiquitin-proteasome pathway, thereby improving motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Additionally, Rosolutamide promotes mitochondrial function, autophagy, and reduces intracellular and mitochondrial reactive oxygen species (ROS) levels, making it a valuable tool for research exploring neurodegenerative diseases and oxidative stress. -
NRF2 Activator
S217879 is a selective NRF2 activator that functions by disrupting the KEAP1-NRF2 interaction with a dissociation constant (Kd) of 4.15 nM. This compound activates the NRF2 pathway, leading to enhanced antioxidant responses. S217879 has demonstrated efficacy in ameliorating steatohepatitis and mitigating liver fibrosis. It is a valuable tool for research focused on metabolic dysfunction-associated steatotic liver disease and nonalcoholic steatohepatitis. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-25 is a potent inhibitor of the Keap1-Nrf2 interaction, exhibiting an IC50 of 0.55 μM and a binding affinity (Kd) of 0.50 μM. This compound effectively activates the Nrf2 pathway, leading to the reduction of reactive oxygen species (ROS) and pro-inflammatory cytokines such as IL-1β and IL-6. Keap1-Nrf2-IN-25 has demonstrated protective effects in models of colitis, particularly against DSS-induced inflammation, making it a valuable tool for research in oxidative stress and inflammatory diseases. -
Nrf2 Inhibitor
Nrf2-IN-3 is a small-molecule inhibitor targeting Nrf2 by enhancing the production of reactive oxygen species (ROS). It specifically binds to KEAP1 mutants, restoring their ability to inhibit Nrf2 and facilitating proteasome-dependent degradation of Nrf2 in cells. This compound has shown potential in sensitizing KEAP1-mutated tumor cells to chemotherapeutic agents such as Cisplatin and Gefitinib, making it a valuable tool for research in cancer therapeutics and Nrf2-related signaling pathways. -
Nrf2 Activator
Nrf2 activator-4 is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 µM. This compound effectively suppresses reactive oxygen species related to oxidative stress in microglial cells. Additionally, Nrf2 activator-4 demonstrates the ability to recover learning and memory impairments in a scopolamine-induced mouse model, making it a valuable tool for research focused on neuroprotection and cognitive function. -
KEAP1-NRF2 Inhibitor
Keap1-Nrf2-IN-14 is a potent inhibitor of the KEAP1-NRF2 interaction, exhibiting an IC50 value of 75 nM and a Kd of 24 nM for KEAP1. This compound promotes the expression of NRF2 target genes, resulting in enhanced antioxidant and anti-inflammatory responses. Keap1-Nrf2-IN-14 is valuable for investigating oxidative stress-related inflammation and exploring therapeutic strategies targeting the KEAP1-NRF2 signaling pathway. -
PPARγ Inhibitor, heme oxygenase-1 Activator, Nrf2 Activator
PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders. -
Keap1/Nrf2/HO-1 Activator
7-Deacetylgedunin is a potent activator of the Keap1/Nrf2/HO-1 signaling pathway. It effectively reduces mortality in mice models induced by lipopolysaccharide (LPS) and demonstrates inhibitory effects on Keap1 expression, leading to the suppression of macrophage proliferation. Additionally, 7-Deacetylgedunin exhibits anti-inflammatory properties both in vitro and in vivo, making it a valuable reagent for research focused on inflammation and oxidative stress. -
Nrf2-ARE Activator
Sesaminol is an oral Nrf2-ARE pathway activator that promotes nuclear translocation of Nrf2 and enhances expression of NQO1, thereby bolstering cellular defense against oxidative stress. This compound has been shown to inhibit 6-OHDA-induced ROS production and apoptosis in SH-SY5Y cells. Additionally, sesaminol demonstrates neuroprotective effects in models of Parkinson's disease induced by Rotenone, making it a valuable tool for research into neuroprotection and oxidative stress response mechanisms. -
NQO1 Inducer
Keap1-Nrf2-IN-10 is a potent inducer of NQO1, mediating the Keap1-Nrf2 signaling pathway. This compound effectively reduces oxidative stress by lowering levels of malondialdehyde (MDA), reactive oxygen species (ROS), and NQO1 in hepatic tissues. Research indicates that Keap1-Nrf2-IN-10 enhances the survival rates of gamma-irradiated mice, making it a valuable tool for studies focused on oxidative damage and cellular protection mechanisms. -
'Nrf2 Activator, ROS Inhibitor'
Ezetimibe ketone is a potent Nrf2 activator and reactive oxygen species (ROS) inhibitor. It effectively reduces H2O2-induced ROS production and mitigates apoptosis in renal tubular epithelial cells. This compound has significant implications for research on renal tubular injury and inflammation. -
PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator
JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms. -
NRF2 Activator
BC-1901S is a proteasome-independent activator and stabilizer of NRF2. It functions by binding to DCAF1, an E3 ligase subunit, disrupting the NRF2/DCAF1 interaction, and inhibiting NRF2 ubiquitination through a KEAP1-independent pathway. BC-1901S demonstrates anti-inflammatory effects in murine models of LPS-induced acute lung injury, making it a valuable tool for research into NRF2-related pathways and inflammation. -
Nrf2 Activator
Ginnalin A, a potent Nrf2 activator, demonstrates significant antiproliferative activity against HCT116, SW480, and SW620 cancer cell lines, with IC50 values of 24.8, 22.0, and 39.7 μM, respectively. This compound induces S phase arrest in cancer cells and activates the p62-Keap1-Nrf2 signaling pathway, leading to the upregulation of mRNA and protein expressions of key protective markers such as Nrf2, HO-1, and NQO1. Additionally, Ginnalin A promotes the translocation of Nrf2 from the cytoplasm to the nucleus, making it a valuable tool for research into colon cancer mechanisms and potential therapies. -
Keap1/S349-p-p62 Interaction Inhibitor
K67 is a selective inhibitor targeting the interaction between Keap1 and S349 phosphorylated p62, with an IC50 of 1.5 μM. This compound demonstrates a weaker inhibitory effect on the Keap1-Nrf2 interaction (IC50 of 6.2 μM) and functions by competitively binding to Keap1's binding site, disrupting the aberrant activation of the p62-dependent Nrf2 pathway. K67 has been shown to inhibit tumor cell proliferation and increase the sensitivity of hepatocellular carcinoma (HCC) cells to chemotherapeutic agents by restoring Keap1-mediated ubiquitination and subsequent degradation of Nrf2. This makes K67 a valuable tool for investigating therapeutic strategies in cancer research. -
AMPK/Nrf2 Activator
Fortunellin is a flavonoid that acts as an AMPK/Nrf2 activator, derived from the fruits of Fortunella margarita (kumquat). It demonstrates minimal toxicity in murine models and effectively reduces inflammation and reactive oxygen species (ROS) generation in H9C2 cells induced by lipopolysaccharide (LPS). By enhancing the AMPK/Nrf2 pathway, Fortunellin protects against fructose-induced inflammation and oxidative stress, making it a valuable tool for research in diabetic cardiomyopathy. -
AMPK/Nrf2 Activator
Ethyl (E)-ferulate is an activator of the AMPK/Nrf2 signaling pathway, demonstrating significant potential in reducing acute lung injury induced by lipopolysaccharide. This compound exhibits antioxidant and free radical scavenging properties, contributing to its anti-inflammatory and neuroprotective effects. Ethyl (E)-ferulate is a valuable tool for research focused on inflammation and neurodegenerative diseases. -
Nrf2 Activator
RA839 is a selective activator of the Nrf2/ARE pathway, functioning as a non-covalent small molecule binder of Keap1 with a Kd of approximately 6 μM. This compound inhibits the expression of inducible nitric oxide synthase and the subsequent release of nitric oxide. RA839 demonstrates significant anti-rotaviral and anti-inflammatory properties, making it a valuable tool for research into oxidative stress, viral infections, and inflammation-related pathways. -
Keap1/Nrf2 Inhibitor
PRL-295 is an orally active inhibitor targeting the interaction between Keap1 and Nrf2. By enhancing the thermal stability of Keap1, PRL-295 disrupts its binding to Nrf2, leading to the activation of Nrf2-dependent genes such as NAD(P)H:quinone oxidoreductase 1 (NQO1). This compound has demonstrated protective effects against Acetaminophen-induced liver injury in murine models, making it a valuable tool for research into oxidative stress and related pathologies. -
Nrf2/AMPK/mTOR Activator
Hydroxycitric acid is an orally active compound that serves as a multifunctional activator of Nrf2, AMPK, and mTOR pathways. It enhances the expression of antioxidant enzymes, such as superoxide dismutase, and increases glutathione levels, thereby mitigating oxidative stress and ferroptosis, particularly in renal tubular epithelial cells. Additionally, hydroxycitric acid induces cell cycle arrest in cancer cells and promotes DNA fragmentation through modulation of the AMPK and mTORC1/S6K signaling pathways. This compound is valuable for research in oxidative stress, cancer biology, and metabolic regulation. -
Nrf2 Pathway Activator
Pyrraline is an Nrf2 pathway activator that enhances antioxidant defenses and mitigates inflammation. It promotes the upregulation of antioxidant enzymes, including NAD(P)H dehydrogenase (NQO1) and heme oxygenase-1 (HO-1), through the activation of the antioxidant response element (ARE), while also inhibiting NFκB-mediated inflammatory pathways. This compound holds significant potential for investigations into metabolic disorders, such as diabetic nephropathy, as well as various cancer research applications. -
NRF2 Glue Degrader
VVD-130037 is a covalent molecular glue and allosteric degrader of NRF2, targeting the KEAP1 protein. By binding to KEAP1, it enhances the formation of the KEAP1-CUL3 E3 ligase complex, leading to increased ubiquitination and subsequent degradation of NRF2. This compound demonstrates KEAP1 target-binding activity in both in vitro assays and mouse models, making it a useful tool in research involving NRF2-dependent cancers, solid tumors with KEAP1 mutations, and advanced solid tumors. -
PGK1 Inhibitor
CBR-470-1 is a selective inhibitor of phosphoglycerate kinase 1 (PGK1), a key enzyme in the glycolytic pathway. This compound also acts as a non-covalent activator of Nrf2, enhancing the cellular defense mechanisms against oxidative stress. In cellular models, CBR-470-1 has demonstrated protective effects against MPP+-induced cytotoxicity in SH-SY5Y neuronal cells by activating the Keap1-Nrf2 signaling pathway. This dual functionality makes CBR-470-1 a valuable tool for research in metabolic regulation and neuroprotection. -
Perfume Analogue
Safranal, the primary aromatic compound derived from Saffron (Crocus sativus), serves as a key target for research involving its neuroprotective and anti-inflammatory properties. Its potential applications in the study of neurodegenerative diseases, particularly Parkinson's disease, make it a valuable reagent for chemical research. Safranal's unique characteristics also support investigations into its effects on sensory perception and mood enhancement. -
Nrf2 Activator
Nrf2 activator-2 (compound O15) is a potent Nrf2 agonist that functions by disrupting the interaction between Keap1 and Nrf2, thereby promoting Nrf2 activation. With an EC50 of 2.9 μM in 293 T cells, this compound significantly reduces the levels of ubiquitinated Nrf2, enhancing its stability and nuclear translocation. Nrf2 activator-2 is valuable in studies exploring oxidative stress response, cellular defense mechanisms, and potential therapeutic applications in diseases associated with Nrf2 dysregulation. -
Keap1-Nrf2 Activator
Dibenzoylmethane is a potent activator of the Keap1-Nrf2 pathway. By promoting the dissociation of Nrf2 from Keap1, it facilitates the nuclear translocation of Nrf2, leading to enhanced expression of antioxidant and cytoprotective genes. This compound has potential applications in cancer prevention research and studies focused on mitigating oxidative stress. -
NRF2/ATF4 Activator
I-152 is a bifunctional conjugate designed as an NRF2 and ATF4 activator. This compound enhances cellular antioxidant responses and promotes cytoprotective signaling pathways. Additionally, I-152 exhibits anti-proliferative properties, making it a valuable tool for research in cancer biology and oxidative stress studies. -
Nrf2 Activator
DDO-7263 is a potent activator of Nrf2, functioning primarily through its binding to Rpn6, which inhibits the assembly of the 26S proteasome and prevents the degradation of ubiquitinated Nrf2. This results in the translocation of Nrf2 into the nucleus, thereby enhancing its transcriptional activity. Additionally, DDO-7263 has been shown to inhibit the activation of the NLRP3 inflammasome, demonstrating significant anti-inflammatory properties. It holds promise for research applications in neurodegenerative diseases, such as Parkinson's disease. -
Nrf2 Activator
Eriodictyol-7-O-glucoside is a flavonoid that functions as an Nrf2 activator. It demonstrates potent scavenging activity against hydroxyl radicals and superoxide anions, with IC50 values of 0.28 mM and 0.30 mM, respectively. This compound enhances the nuclear localization of Nrf2, leading to the induction of Nrf2/ARE-dependent gene expression. Eriodictyol-7-O-glucoside offers protective effects against oxidative stress induced by oxygen and glucose deprivation, and exhibits neuroprotective properties in models of focal cerebral ischemia. It is valuable for research in stroke and neuroprotection studies. -
NRF2 Activator
Monoethyl fumarate is the monoethyl ester of fumaric acid and serves as an activator of the Nrf2 pathway. This compound exhibits significant potential for antioxidant activity and may play a crucial role in cellular defense mechanisms. Its applications extend to research involving neuroprotection and inflammation modulation, as well as in the exploration of therapeutic strategies for various diseases. Additionally, monoethyl fumarate is utilized as a preservative and polymerization agent for macromolecular materials. -
Keap1-Nrf2 PPI Inhibitor
NXPZ-2 is an orally active inhibitor of the Keap1-Nrf2 protein-protein interaction with a Ki value of 95 nM and EC50 values of 120 and 170 nM. It has demonstrated the ability to dose-dependently mitigate Aβ[1-42]-induced cognitive dysfunction and improve brain tissue pathology in Alzheimer's disease models by enhancing neuronal quantity and function. NXPZ-2 functions by inhibiting oxidative stress through increased expression of Nrf2 and promoting its translocation from the cytoplasm to the nucleus, supporting research into Keap1-Nrf2 interactions and Alzheimer’s disease. -
Nrf2 Activator
Nrf2 activator-3 is a potent activator of the NF-E2-related factor 2 (Nrf2) pathway. This compound enhances antioxidant response element (ARE) transcriptional activity, promoting the expression of various cytoprotective genes. Nrf2 activator-3 is primarily utilized in research focusing on cerebral ischemic injury, where it may help elucidate mechanisms of neuroprotection and potential therapeutic strategies. -
NRF2 Activator
CBR-470-2 is a glycine-substituted analog that functions as an NRF2 activator. This compound significantly enhances NRF2 signaling pathways, making it a valuable tool for research into metabolic modulation, particularly glycolysis. Its ability to influence key cellular processes positions CBR-470-2 as an important reagent for exploring the roles of oxidative stress and inflammation in various biological systems. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-13 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), exhibiting an IC50 of 0.15 μM. This compound effectively disrupts the binding of Keap1 to Nrf2 by establishing hydrogen bonds with critical polar residues such as Asn414, Arg415, Arg483, and Gln530. Keap1-Nrf2-IN-13 is valuable for research focused on oxidative stress-related conditions and inflammatory diseases, including pulmonary fibrosis, chronic obstructive pulmonary disease (COPD), and various cancers. -
Keap1-Nrf2 Inhibitor
Toralactone is a selective inhibitor of the Keap1-Nrf2 pathway, which plays a crucial role in cellular antioxidant defense mechanisms. Originating from Cassia obtusifolia, Toralactone exhibits significant hepatoprotective effects mediated through Nrf2 activation. This compound is suitable for research applications focused on oxidative stress, hepatotoxicity, and the modulation of antioxidant responses in various biological systems. -
Keap1-Nrf2 Inhibitor
Nrf2 activator-12 is a potent activator of the Keap1-Nrf2 pathway, with an EC50 value of 83.5 nM. This compound demonstrates significant pharmacological effects, including the ability to reverse disease progression and mitigate demyelination in an experimental autoimmune encephalomyelitis mouse model. Nrf2 activator-12 is valuable for studies exploring oxidative stress responses and potential neuroprotective strategies in various neurological disorders. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-9 is a selective inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI) with a reported IC50 of 0.575 μM. This compound enhances the expression of Nrf2 target genes, including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and the modulatory and catalytic subunits of glutamate-cysteine ligase (Gclc and Gclm). Keap1-Nrf2-IN-9 exhibits low cytotoxicity in ARPE19 cells, making it a valuable tool for studies focused on oxidative stress and cellular defense mechanisms. -
Nrf2 Activator
Nrf2 activator-1 is a potent activator of the NF-E2 related factor 2 (Nrf2), a key regulator of cellular antioxidant response. It demonstrates significant biological activity in modulating oxidative stress and inflammation. This compound is valuable for research applications related to chronic obstructive pulmonary disease (COPD), asthma, acute lung injury (ALI), acute respiratory distress syndrome (ARDS), and pulmonary fibrosis, facilitating the exploration of therapeutic interventions in these conditions. -
NRF2 Activator
MIND4-17 is a selective NRF2 activator that covalently modifies the C151 residue of Keap1. By disrupting the association between Keap1 and Nrf2, MIND4-17 promotes Nrf2 protein stabilization and subsequent nuclear translocation, enhancing the cellular antioxidant response. This compound demonstrates strong antioxidant activity and is valuable for research applications focused on oxidative stress and related pathways. -
Keap1-Cul3 E3 ligase Complex Allosteric Molecular Glues
VVD 065 is an allosteric modulator of the Keap1-Cul3 E3 ligase complex that functions as a molecular glue. By activating KEAP1, VVD 065 promotes the degradation of NRF2, an essential regulator of antioxidant defenses. This compound has demonstrated the ability to inhibit tumor growth in non-small cell lung cancer and esophageal squamous cell carcinoma xenograft models. VVD 065 serves as a valuable tool for research on cancer biology and therapeutic strategies targeting oxidative stress responses. -
NR0B1-protein Interactions Destructive Agent
BPK-29 hydrochloride is a selective agent that disrupts interactions between the atypical orphan nuclear receptor NR0B1 and its protein partners, such as RBM45 and SNW1, through covalent modification of cysteine residue C274. This compound has been shown to inhibit anchorage-independent growth in KEAP1-mutant cancer cell lines, making it a valuable tool for studying the biological functions of NR0B1 and its role in cancer development. BPK-29 hydrochloride is essential for research on targeted therapies in oncology and the mechanisms underlying cancer cell proliferation. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-7 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), exhibiting an IC50 value of 0.45 µM. This compound plays a crucial role in modulating the Nrf2 signaling pathway, which is essential for cellular responses to oxidative stress. Its application is significant in studies focused on neuroprotection, cancer therapy, and various diseases associated with oxidative damage. -
Nrf2 Peptide
Nrf2 (69-84) is a peptide derived from the Nrf2 protein, featuring the essential ETGE motif critical for binding to the Kelch domain of the Keap1 protein. This peptide serves as a valuable tool for investigating the regulatory functions of Nrf2 in various biological processes, particularly in the context of cancer, neurodegenerative disorders, and inflammatory diseases. Its application aids in elucidating the mechanisms by which Nrf2 modulates cellular responses to oxidative stress and inflammation. -
Nrf2 Activator
Nrf2-Activator-12G is a potent activator of Nrf2, a critical transcription factor involved in cellular antioxidant defense mechanisms. This compound effectively induces the expression of Nrf2-dependent antioxidant enzymes at the mRNA and protein levels in dopaminergic neuronal cells. Nrf2-Activator-12G is applicable in research related to Parkinson's Disease, facilitating studies on oxidative stress and neuroprotection. -
Nrf2/ARE Pathway Activator
(R)-5-Hydroxy-1,7-diphenyl-3-heptanone is a diarylheptanoid that serves as an activator of the Nrf2/ARE signaling pathway. This compound demonstrates significant antioxidant properties, alleviating oxidative stress and improving insulin resistance. Its role in enhancing cellular defense mechanisms makes it valuable for research in metabolic disorders and oxidative stress-related conditions. -
Keap1-Nrf2 Activator
Dimethyl fumarate-d6 is a deuterium-labeled derivative of Dimethyl fumarate, functioning as a Keap1-Nrf2 pathway activator. This compound enhances the expression of antioxidant genes by stimulating the Nrf2 signaling pathway, thereby providing potential protective effects against oxidative stress. It is useful in research focused on oxidative stress, inflammation, and cellular response mechanisms. -
Anticancer Agent
Tigloylgomisin H is a lignan that targets the induction of quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. This compound functions as a monofunctional inducer, specifically enhancing the expression of the phase II detoxification enzyme NQO1 via the NF-E2-related factor 2 (Nrf2)-ARE pathway. As a result, Tigloylgomisin H demonstrates potential as a preventive agent against liver cancer, making it valuable for cancer research applications.
