Catalog No.
Product Name
Application
Product Information
Citations
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Nrf2 inhibitor
RTA-408 is a synthetic triterpenoid that potently activates the antioxidative transcription factor Nrf2 and inhibits the proinflammatory transcription factor NF-kB. -
NRF2 inhibitor
ML-385 is an inhibitor of nuclear factor erythroid 2-related factor 2 (Nrf2) with IC50 value of 1.9 μM.- Liping Luo, .et al. , Heliyon, 2023, Aug 3;9(8):e18929 PMID: 37600361
- Methionine is a sulfur-containing essential L-amino acid that is important in many body functions.
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Keap1-Nrf2 inhibitor
Keap1-CNrf2-IN-1 (compound35) is a Kelch-like ECH-associated protein 1-nuclear factor erythroid 2-related factor 2 (Keap1-Nrf2) protein-protein interaction inhibitor, and with an IC50 of 43 nM for Keap1 protein. - 4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
- CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB.
- Diroximel fumarate (DRF) is a prodrug of monomethyl fumarate in a controlled-release formulation that rapidly and efficiently converts to MMF in the body.
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Keap1/Nrf2/ARE pathway inducer
(R)-Sulforaphane is a highly potent inducer of the Keap1/Nrf2/ARE pathway. (R)-Sulforaphane is a far more potent inducer of the carcinogen-detoxifying enzyme systems in rat liver and lung than the S-isomer.- Isin Cakir, .et al. , Elife, 2022, Mar 24 PMID: 35323110
- β-Thujaplicin is a toxic tropolone derivative present in the heartwood of western red cedar (Thuja plicata) and is used as a preservative and antimicrobial additive in a number of commercial goods.
- KI696 isomer is the less active isomer of KI696. KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
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HDAC inhibitor
Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.- Satoshi Endo, .et al. , J Biochem, 2021, Mar 17 PMID: 33729485
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antioxidant agent
Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway. -
Heme oxygenase-1 inducer
Coniferaldehyde (Ferulaldehyde), isolated from the ethanol extract of Vitex rotundifolia fruits, is an effective inducer of heme oxygenase-1 (HO-1). - 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 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. -
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/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. -
Nrf2 Inhibitor
Nrf2-IN-4 is a potent Nrf2 inhibitor that induces ferroptosis through the inhibition of the Nrf2 pathway. By disrupting iron homeostasis and facilitating ferritin degradation, Nrf2-IN-4 triggers ferroptotic cell death. Additionally, it promotes lysosome activation by enhancing iron-dependent reactive oxygen species (ROS) production and acidification. Due to its significant antitumor efficacy, Nrf2-IN-4 is a valuable tool for studying breast cancer and exploring therapeutic strategies targeting the Nrf2 pathway. -
Nrf2 Activator/ROS Inhibitor
L-Cystine is an effective Nrf2 activator and reactive oxygen species (ROS) inhibitor. This extracellular form of L-Cysteine elevates Nrf2 protein expression and facilitates its transcriptional activity, thereby reducing ROS generation and providing protection against oxidant- or Doxorubicin-induced apoptosis. Additionally, L-Cystine has been shown to enhance antigen-specific IgG production and T helper 2 mediated responses through increased glutathione levels in murine models. This makes L-Cystine a valuable reagent for research in cystinuria and kidney stone formation. -
Nrf2-Gpx4 Activator
Gingerenone A is an Nrf2-Gpx4 activator that triggers ferroptosis in liver tissue, demonstrating significant potential for therapeutic intervention in liver damage. This compound exhibits notable anti-inflammatory, anti-diabetic, anti-tumor, and pro-aging properties observed in murine models, making it valuable for research in oxidative stress regulation and associated diseases. Its oral bioactivity further enhances its applicability in in vivo studies. -
Endogenous Metabolite; Nrf2 Activator; ROS Inhibitor
L-Cystine hydrochloride is an endogenous metabolite that serves as a potent Nrf2 activator and reactive oxygen species (ROS) inhibitor. It enhances Nrf2 protein expression, facilitating transcriptional responses that combat oxidative stress. Research indicates that L-Cystine hydrochloride reduces ROS generation and protects cells from apoptosis induced by oxidants or Doxorubicin. Additionally, its combination with L-theanine has been shown to boost antigen-specific IgG production by elevating glutathione levels and promoting T helper 2 (Th2) responses. This compound has significant potential for studying cystinuria and kidney stone formation. -
Keap1/Nrf2 Activator
Sweroside, a potent Keap1/Nrf2 activator, is an iridoid glycoside that enhances Nrf2 nuclear translocation by competing with Keap1. This compound exhibits diverse biological activities, including antioxidant, anti-inflammatory, and anti-apoptotic effects, while regulating lipid metabolism. Sweroside's ability to inhibit oxidative stress and NLRP3-mediated pyroptosis, alongside its activation of the SIRT1 and AMPK/mTOR pathways, makes it valuable for investigating conditions such as myocardial ischemia-reperfusion injury, leukemia, acute lung injury, and non-alcoholic fatty liver disease. -
Keap1-Nrf2 Agonist
Methyl 3,4-dihydroxybenzoate functions as a Keap1-Nrf2 agonist, promoting the activation of the Nrf2 pathway. This compound exhibits significant antioxidant and anti-inflammatory properties, making it valuable in research focused on oxidative stress and cellular defense mechanisms. It is primarily utilized in studies investigating the neuroprotective effects of polyphenols and their potential therapeutic applications in various diseases. -
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
Sarmentosin is a potent activator of the Nrf2 pathway, which plays a crucial role in cellular defense against oxidative stress. This compound has been shown to inhibit mTOR signaling and promote autophagy-dependent apoptosis in human hepatocellular carcinoma (HCC) cells. Its ability to modulate these critical pathways makes Sarmentosin a valuable tool for research into cancer biology and potential therapeutic strategies. -
Nrf2 Activator
Nrf2 Activator-10 (Compound AI-1) acts as a PI3K-dependent inducer of the antioxidant response element (ARE), with an EC50 value of 2.7 μM, effectively activating Nrf2. By modifying Keap1 and inhibiting the Cul3-Keap1 ubiquitin ligase complex, Nrf2 Activator-10 enhances Nrf2 transcription and promotes cellular defense mechanisms. This compound is particularly valuable for research focused on oxidative stress and cytoprotection, demonstrating protective effects against H2O2-induced apoptosis. -
NF-κB Inhibitor/Nrf2/AMPK Activator
Panduratin A is a potent inhibitor of the NF-κB signaling pathway, recognized for its significant anti-inflammatory and antioxidant properties. It demonstrates protective effects against nephrotoxicity induced by Colistin, primarily by mitigating oxidative stress and enhancing mitochondrial function. Additionally, Panduratin A activates autophagy through an AMPK-dependent mechanism and exhibits potential anti-tuberculosis and antiviral activities by inhibiting the methyltransferase of SARS-CoV-2. These diverse biological activities make Panduratin A a valuable tool in various areas of research, including inflammation, cellular stress responses, and infectious diseases. -
Nrf2 activator
Nrf2 activator-11 is a potent Nrf2 activator that demonstrates blood-brain barrier permeability. This compound exhibits significant biological activities, including antioxidant, anti-inflammatory, anti-ferroptotic, and anti-apoptotic effects. Nrf2 activator-11 is particularly valuable for research involving cerebral ischemia-reperfusion injury models, providing insights into neuroprotective mechanisms and therapeutic interventions. -
Keap1-Nrf2 Protein-Protein Inhibitor
CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting an IC50 of 0.63 µM. This compound demonstrates significant anti-inflammatory and antioxidant properties by activating the Nrf2-dependent pathway and inhibiting the NF-κB-related inflammatory response. CPUY192018 is ideal for research applications focused on inflammation-related diseases and the modulation of oxidative stress. -
Nrf2 Activator
Artemisitene is a natural derivative of Artemisinin that functions as a Nrf2 activator. It enhances antioxidant and anticancer activities by reducing Nrf2 ubiquitination, thereby increasing its stability. This compound is utilized in research focused on oxidative stress, cancer biology, and the modulation of cellular defense mechanisms. -
Keap1-Nrf2 PPI Inhibitor
Tricetin is a competitive inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI). This compound exhibits neuroprotective effects by activating the Nrf2/HO-1 signaling pathway, which mitigates 6-OHDA-induced neurotoxicity in models of Parkinson's disease. Its mechanism of action helps to prevent apoptosis through mitochondrial pathways, making it a valuable reagent for research into neurodegenerative diseases and oxidative stress response. -
Keap1-Nrf2 Activator
CDDO-TFEA is a trifluoroacetamide derivative of CDDO and serves as a potent Keap1-Nrf2 activator. This compound effectively enhances Nrf2 expression and signaling in various models of neurodegenerative diseases, such as multiple sclerosis, amyotrophic lateral sclerosis, and Huntington's disease. In cancer research, CDDO-TFEA demonstrates significant biological activity by inducing apoptosis and inhibiting colony formation in Ewing's sarcoma and neuroblastoma cell lines, with IC50 values ranging from 85 to 170 nM. -
Nrf2 Activator
Danshensu sodium, a phenolic compound, serves as an Nrf2 activator, effectively inducing the Nrf2/HO-1 signaling pathway while inhibiting NF-κB activity. It diminishes reactive oxygen species (ROS) production, enhances antioxidant defenses, and suppresses intrinsic apoptosis. Additionally, Danshensu sodium exhibits significant antiviral properties against SARS-CoV-2, with an EC50 value of 0.97 μM. This compound is valuable for researching its anti-oxidative, anti-inflammatory, and anti-apoptotic effects, holding potential implications for COVID-19, cardiovascular, and cerebrovascular diseases.
