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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
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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. -
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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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
'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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
