Catalog No.
Product Name
Application
Product Information
Citations
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Keap1-Nrf2 Probe
Keap1-Nrf2 Probe is designed to selectively bind to the Kelch-like ECH-associated protein 1 (Keap1), modulating the nuclear factor erythroid 2-related factor 2 (Nrf2) signaling pathway. By inhibiting Keap1 function, this probe enhances the transcription of antioxidant response elements, promoting cellular defense against oxidative stress. It is valuable for research on oxidative stress-related diseases, drug discovery targeting the Nrf2 pathway, and studying cellular mechanisms involved in stress responses. -
Nrf2 Activator
Rosolic acid is a potent activator of Nrf2, leading to the upregulation of its downstream targets. This compound has been shown to enhance levels of angiogenic factors while reducing inflammation markers such as TNF-α and IL-1β, as well as apoptotic markers like CXCL10 and CCL2. Additionally, rosolic acid aids in restoring pancreatic cell function and offers protective effects on endothelial cells against endoplasmic reticulum stress. Its applications include studies on oxidative stress, inflammation modulation, and cellular protection mechanisms. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-8 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, demonstrating IC50 values of 64.5 nM and 14.2 nM in fluorescence polarization and time-resolved fluorescence resonance energy transfer assays, respectively. This compound effectively enhances the mRNA expression of key Nrf2 target genes, including GSTM3, HMOX2, and NQO1. Keap1-Nrf2-IN-8 is instrumental in research focused on oxidative stress response and cellular defense mechanisms. -
Nrf2 Activator
2-Trifluoromethyl-2'-methoxychalcone is a chalcone derivative that functions as a potent activator of the Nrf2 pathway. This compound promotes the expression of antioxidant proteins and plays a crucial role in cellular protection against oxidative stress. It is particularly relevant for research applications focused on diseases linked to oxidative stress and inflammation. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-15 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting IC50 values of 77 nM in fluorescence polarization (FP) assays and 2.5 nM in time-resolved Förster resonance energy transfer (TR-FRET) assays. This compound enhances the activation of the Nrf2 pathway, which plays a critical role in cellular defense mechanisms against oxidative stress and inflammation. Keap1-Nrf2-IN-15 is a valuable tool for research applications focused on neuroprotection, cancer therapy, and the modulation of antioxidant responses. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-12 is a potent inhibitor of the Keap1-Nrf2 interaction, exhibiting an IC50 value of 2.30 µM. This compound effectively modulates the Nrf2 signaling pathway, which is critical for cellular defense against oxidative stress. Additionally, Keap1-Nrf2-IN-12 demonstrates metabolic stability in human liver microsomes, making it a valuable tool for research applications focused on oxidative stress response and related therapeutic targets. -
Flavone Glycoside
Carlinoside is a flavone glycoside that exhibits hepatoprotective properties. It effectively reduces hepatic bilirubin accumulation by enhancing bilirubin-UDP-glucuronosyltransferase (UGT) activity through the activation of Nrf2 gene expression. This compound holds potential for the management of hyperbilirubinemia associated with liver dysfunction. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-22 is a selective inhibitor of the Keap1-Nrf2 interaction, exhibiting a KD2 value of 42.2 nM for Keap1. This compound is valuable for investigating the regulatory mechanisms of oxidative stress and cytoprotection in cellular environments. Key research applications include the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury, where modulation of the Nrf2 pathway may provide therapeutic insights. -
KEAP1 Inhibitor
Keap1-IN-2 is a potent KEAP1 inhibitor with an IC50 of 2 nM, designed to indirectly activate Nrf2. By inhibiting KEAP1, this compound enhances cellular antioxidant capacity and promotes the accumulation and nuclear translocation of Nrf2, preventing its degradation. Keap1-IN-2 is applicable in research exploring diseases linked to oxidative stress, including inflammatory bowel disease, Crohn's disease, and immune disorders such as ulcerative colitis. -
Nrf-2 Activator
TPNA10168 is an Nrf-2 activator that enhances the Keap1-Nrf2-ARE signaling pathway. It exhibits neuroprotective properties against oxidative stress-induced cellular damage and significantly downregulates the expression of inflammatory genes such as TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 is suitable for research applications focused on anti-inflammatory responses and neurological disorders. -
Antioxidant Agent
WN1316 is an orally active antioxidant agent that exhibits neuroprotective properties. It is primarily utilized in research focused on amyotrophic lateral sclerosis (ALS), making it a valuable tool for studying neurodegenerative diseases and the underlying mechanisms of oxidative stress in neuronal cells. -
Nrf2 Activator
CPDT is a potent activator of the transcription factor Nrf2, which plays a crucial role in cellular defense mechanisms. It significantly induces the expression of phase 2 enzymes, including glutathione S-transferase, NAD(P)H:quinone:oxidoreductase 1, and glutamate cysteine synthetase. Research demonstrates that CPDT enhances glutathione levels in rat bladder in vivo and in cultured bladder cells in vitro, highlighting its potential applications in studies of oxidative stress and antioxidant responses. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-17 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction. This compound enhances the activation of the Nrf2 pathway, which plays a critical role in cellular defense against oxidative stress and inflammation. Keap1-Nrf2-IN-17 is valuable for research applications focused on understanding the mechanisms of oxidative stress response and exploring therapeutic options for related diseases. -
BChE Inhibitor
S21-1011 is a selective inhibitor of butyrylcholinesterase (BChE) with IC50 values of 0.059 μM for equine BChE and 0.162 μM for human BChE. This compound demonstrates effective blood-brain barrier permeability and favorable pharmacokinetic properties. Additionally, S21-1011 exhibits anti-inflammatory activity by activating the keap1-Nrf2-ARE signaling pathway, with an EC50 of 23.48 μM for antioxidant response element activation. Its potential to ameliorate cognitive impairments in murine models of Alzheimer’s disease makes it relevant for neurodegenerative research applications. -
AChE/Nrf2 Modulator
AChE/Nrf2 Modulator 1 is an orally active compound that targets both acetylcholinesterase (AChE) and the nuclear factor erythroid 2-related factor 2 (Nrf2). It exhibits significant Nrf2 inductive activity along with potent AChE inhibitory effects, presenting IC50 values of 0.07 μM for eel AChE and 0.38 μM for human AChE. This compound is primarily utilized in research focused on Alzheimer's disease, providing insights into neuroprotective mechanisms and cholinergic system modulation. -
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. -
Isomer
(R,S,R)-ML334 is the isomer of ML334, serving as a valuable experimental control in research. This compound acts primarily as a cell-permeable activator of NRF2 by inhibiting the Keap1-NRF2 protein-protein interaction. With a binding affinity of 1 µM to the Kelch domain of Keap1, (R,S,R)-ML334 enhances NRF2 expression, promotes its nuclear translocation, and induces antioxidant response elements (ARE) activity, making it significant for studies related to oxidative stress and cellular defense mechanisms. -
Anti-inflammatory Agent
Chikusetsusaponin IVa is an orally active anti-inflammatory agent that targets YAP, demonstrating a binding affinity with a KD value of 0.388 mM. This compound effectively reduces the expression of inflammatory mediators such as IL-6, IL-10, and COX-2, while modulating nitric oxide production and promoting reactive oxygen species generation. Additionally, Chikusetsusaponin IVa induces apoptosis, inhibits MAPK and TAZ signaling pathways, and regulates Nrf2 and JAK/STAT pathways. It exhibits potential as an anti-H9N2 avian influenza virus agent and demonstrates anti-cancer properties, along with hepatoprotective and osteoprotective effects, making it a valuable tool for research in inflammation and cancer biology. -
Nrf2 Degrader
Nrf2 Degrader 1 is a potent PROTAC that targets and degrades Nrf2, a key regulator of antioxidant response and cell survival. This compound demonstrates significant anticancer activity, effectively inhibiting the growth of A549 and LK-2 cancer cell lines with IC50 values of 100 nM and 40 nM, respectively. It is a valuable tool for studying the role of Nrf2 in cancer biology and has potential applications in therapeutic development. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
Antiviral Agent
Dendrobine is an alkaloid derived from Dendrobium nobile, primarily targeting viral infections as an antiviral agent. It demonstrates significant antiviral activity against influenza A viruses, exhibiting IC50 values of 3.39 μM, 2.16 μM, and 5.32 μM for strains A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1), and A/Aichi/2/68 (H3N2), respectively. Additionally, Dendrobine activates the JNK/p38/Nrf2 signaling pathway and possesses various biological properties, including antitumor, anti-inflammatory, and neuroprotective effects, making it valuable in diverse research applications. -
Nrf2 Activator
Nrf2 activator-21 is a potent activator of the Nrf2 pathway, which disrupts the Keap1-Nrf2 interaction, thereby promoting antioxidant defense mechanisms. This compound exhibits dual antioxidant and neuroprotective properties, significantly reducing apoptosis and caspase-3 activity in hippocampal neurons. Nrf2 activator-21 effectively targets cerebral ischemia/reperfusion injury (CIRI), enhancing neurological function, alleviating anxiety-like behavior, and improving memory in rat models subjected to 2-vessel occlusion (2VO). It serves as a valuable tool for investigating the therapeutic potential of Nrf2 activation in cerebral ischemic conditions. - 7-Hydroxyflavone is an orally active flavonoid isolated from *Clerodendrum phlomidis*, exhibiting notable anti-inflammatory activity. It protects renal cells from nicotine-induced cytotoxicity through activation of the ERK/Nrf2/HO-1 signaling pathway. Additionally, 7-Hydroxyflavone inhibits PKM2 with an IC50 of 2.12 μM, and suppresses COX-2 and 5-LOX with IC50 values of 27 μg/mL and 33 μg/mL, respectively.
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ERK MAPK Modulator
ACA-28 (compound 2a) is a potent modulator of the ERK MAPK signaling pathway that exerts anticancer effects through a unique mechanism involving ERK hyperactivation. Rather than inhibiting ERK activity directly, ACA-28 induces sustained ERK activation, which paradoxically triggers apoptosis in cancer cells. It demonstrates selective cytotoxicity, inhibiting the growth of melanoma cells (SK-MEL-28) with an IC₅₀ of 5.3 μM, while showing lower toxicity toward normal human melanocytes (NHEM), with an IC₅₀ of 10.1 μM. ACA-28's ability to exploit ERK signaling dysregulation for selective induction of apoptosis makes it a promising candidate for further development in cancer therapy, particularly in ERK-dependent malignancies. -
Nrf2/HO-1 Activator
Nrf2/HO-1 activator 2 is a difluoro-substituted compound that functions as a potent activator of the Nrf2/HO-1 signaling pathway. It exhibits neuroprotective and antioxidant properties by promoting the phosphorylation of ERK1/2, JNK, and Akt, particularly in PC12 cells. This compound is valuable for research on neurodegenerative conditions, including Parkinson's disease. -
Keap1/Nrf2/ARE Activator
Keap1/Nrf2/ARE Activator 2 is a potent activator of the Keap1/Nrf2/ARE signaling pathway, promoting Nrf2 nuclear translocation. This compound has been demonstrated to upregulate antioxidant genes, thereby enhancing cellular defense against oxidative stress. Additionally, it exhibits significant neuroprotective effects against H2O2- and Scopolamine-induced neuronal injury in PC12 cells, as well as alleviating memory impairment and neuroinflammation associated with cognitive dysfunction in zebrafish models. Keap1/Nrf2/ARE Activator 2 is a valuable tool for research into Alzheimer's disease and associated neurodegenerative conditions. -
Nrf2 Activator
Dimethyl fumarate is an orally bioavailable Nrf2 activator that enhances the expression of antioxidant genes. This compound has been shown to induce necroptosis in colon cancer cells via mechanisms involving glutathione depletion, reactive oxygen species elevation, and activation of MAPK pathways. Additionally, Dimethyl fumarate promotes autophagy and is applicable in studies focused on multiple sclerosis and related neurodegenerative conditions. -
Nrf2 Activator
Raffinose serves as an Nrf2 activator and is known for its ability to modulate intestinal flora. It inhibits the TLR4-MyD88-NF-κB signaling pathway while promoting Nrf2 signaling, contributing to its anti-inflammatory, antioxidant, and immunomodulatory properties. This compound is orally active and is valuable in research applications focusing on inflammation and oxidative stress. -
Nrf2 Activator/ROS Inhibitor
L-Cystine disodium monohydrate primarily functions as an Nrf2 activator and ROS inhibitor. It elevates Nrf2 protein expression and activates the Nrf2 transcription factor, leading to reduced reactive oxygen species (ROS) generation and protection against apoptosis caused by oxidants and Doxorubicin. Additionally, when combined with L-theanine, it enhances the production of antigen-specific IgG by increasing glutathione levels and promoting T helper 2-mediated responses in mice. This compound is valuable for research into cystinuria and the molecular mechanisms underlying kidney stone formation.
