Catalog No.
Product Name
Application
Product Information
Citations
- 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. -
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
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. -
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. -
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 Activator
ML334 is a potent NRF2 activator that functions by inhibiting the Keap1-NRF2 protein-protein interaction. With a binding affinity to the Keap1 Kelch domain of 1 μM, ML334 effectively promotes NRF2 expression and its subsequent nuclear translocation, thereby enhancing antioxidant response element (ARE) activity. This compound is valuable for research applications focused on oxidative stress, neuroprotection, and cellular responses to environmental stimuli. -
Nrf2 Activator
Nrf2 activator-6 is a tetrahydroisoquinoline compound that functions as an activator of the Nrf2 pathway. It exhibits an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction, thereby promoting the transcriptional activation of antioxidant response elements. This compound is valuable in research applications focused on oxidative stress, inflammation, and neuroprotection. -
Nrf2 activator
Nrf2 activator-7 is a potent activator of the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. By significantly enhancing Nrf2 signaling, it promotes the expression of antioxidant and cytoprotective genes. This reagent is valuable in research focused on oxidative stress, inflammation, and cellular defense mechanisms. -
Capsaicinoid Analog
Nordihydrocapsaicin is a capsacinoid analog known for its pungent properties and oral bioactivity. This compound exhibits potential anti-cancer activities and is derived from both fresh and processed peppers. It may induce a burning sensation upon consumption, making it relevant for research in pain mechanisms and anti-tumor effects. -
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. -
Keap1-Nrf2 Activator
LMDP10 is an orally active 3-amino quinazoline derivative that functions as a Keap1-Nrf2 activator. By binding to Keap1, LMDP10 disrupts the Keap1-Nrf2 interaction, leading to the activation of the Nrf2 pathway. This compound enhances the levels of Nrf2, superoxide dismutase (SOD), and glutathione (GSH), while decreasing malondialdehyde (MDA) and tumor necrosis factor-alpha (TNF-α) levels. LMDP10 exhibits potential in mitigating neurodegeneration and improving cognitive function in models of Alzheimer's disease, making it a valuable tool for research in neurodegenerative disorders. -
Bioactive Peptide
Keap1-Nrf2-IN-16 is a bioactive peptide that targets the KEAP1 protein to disrupt its interaction with the Nrf2 transcription factor. This inhibition leads to the stabilization and activation of Nrf2, promoting the expression of antioxidant response elements and enhancing cellular defense mechanisms. Keap1-Nrf2-IN-16 is utilized in research applications related to oxidative stress, cellular protection, and neurodegenerative diseases. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-23 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, exhibiting an IC50 of 16.0 nM. It demonstrates strong binding affinity to Keap1 with a Kd value of 3.07 nM, making it a valuable tool for research into antioxidant response pathways. This compound is suitable for studies related to cellular defense mechanisms and may have applications in the field of cancer research and neurodegenerative diseases. -
Ligand for Target Protein for PROTAC
Nrf2 activator-22 is a ligand specifically targeting the Nrf2 protein, playing a crucial role in the development of PROTAC-based therapeutics. This compound facilitates the synthesis of PROTAC K-Ras Degrader-7, highlighting its potential in targeted protein degradation research. Nrf2 activator-22 is valuable for studies aimed at manipulating oxidative stress responses and related signaling pathways. -
Nrf2 Activator
Nrf2 activator-5 is a potent activator of the nuclear factor erythroid 2-related factor 2 (Nrf2) pathway. This compound effectively reduces hydrogen peroxide-induced oxidative stress and lipopolysaccharide (LPS)-induced inflammation in BV-2 microglial cells. Nrf2 activator-5 demonstrates significant antioxidant and anti-inflammatory properties, making it valuable for research into neuroinflammation and oxidative stress. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-3 is a selective inhibitor targeting the KEAP1-NRF2 protein-protein interaction, demonstrating a Kd value of 2.5 nM for KEAP1. This compound enhances NRF2 activity, leading to elevated expression of antioxidant response genes. It is valuable for research applications focused on oxidative stress, cancer biology, and neuroprotection, providing insights into mechanisms influencing cellular defense pathways. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-28 is a potent inhibitor of the Keap1-Nrf2 signaling pathway. This compound exhibits significant antioxidant activity by promoting the upregulation of Nrf2 and its downstream targets, including HO-1, GCLM, and Akr1c1. Additionally, Keap1-Nrf2-IN-28 has been shown to mitigate acute liver injury induced by acetaminophen, making it a valuable tool in research related to oxidative stress and liver protection. -
Nrf2 Activator
Fraxinellone analog 1 is a potent Nrf2 activator that enhances the antioxidant defense system and protects against glutamate-mediated excitotoxicity. This compound induces the expression of key antioxidant genes, including Gpx4, Sod1, and Nqo1, demonstrating neuroprotective effects and regulatory capabilities against oxidative stress and inflammation. Fraxinellone analog 1 is valuable for research applications focused on neurodegenerative diseases and related oxidative stress models. -
Keap1-Nrf2 PPI Inhibitor
Keap1-Nrf2-IN-5 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI), with an IC50 of 4.1 µM and a Kd of 3.7 µM. This compound enhances Nrf2 activity, promoting the expression of antioxidant and cytoprotective genes. It serves as a valuable tool for research into oxidative stress, neuroprotection, and cancer therapeutics. -
Nrf2 Activator
Nrf2 activator 17 is a potent activator of the Nrf2 signaling pathway, functioning by inhibiting the interaction between Keap1 and Nrf2 with an IC50 of less than 0.1 pM. This compound demonstrates significant biological activity, exhibiting an EC50 of less than 10 µM in HepG2 cells. Nrf2 activator 17 is utilized in research applications focused on oxidative stress, cellular protection, and the study of Nrf2-related pathways in various disease models. -
Nrf2 Activator
Nrf2 activator-20 is a potent Nrf2 activator that enhances anti-inflammatory and antioxidant responses by disrupting the Keap1-Nrf2 interaction. It has demonstrated beneficial effects in vivo, making it suitable for research applications involving acute respiratory distress syndrome (ARDS) and ischemia-reperfusion injury. This reagent serves as a valuable tool for studying the modulation of oxidative stress and inflammation pathways in various biological contexts. -
Nrf2 Activator
R079 is a selective, orally active Nrf2 activator that enhances Nrf2 translocation with an EC50 of 32.41 μM. By activating Nrf2, R079 effectively neutralizes excess reactive oxygen species, contributing to its anti-inflammatory properties. This compound serves as a valuable tool for research into oxidative stress and inflammatory conditions, including multiple sclerosis. -
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.
