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Pathways Recommended: MAPK/ERK Pathway
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Keap1-Nrf2 pathway activator

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29

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9

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1

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13755
    Sulforaphane
    Maximum Cited Publications
    69 Publications Verification

    		 HDAC Keap1-Nrf2 Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species (ROS) Inflammation/Immunology Cancer
    Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .
    Sulforaphane
  • HY-N0147
    Rutaecarpine
    5+ Cited Publications

    Rutecarpine

    		 COX Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine
  • HY-113298
    Citraconic acid
    4 Publications Verification

    Methylmaleic acid

    		 NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Citraconic acid (Methylmaleic acid) is an orally active inhibitor targeting the NLRP3 inflammasome and Keap1-Nrf2 pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052) .
    Citraconic acid
  • HY-N0806
    Sweroside
    3 Publications Verification

    		 Keap1-Nrf2 AMPK Sirtuin NF-κB NOD-like Receptor (NLR) Pyroptosis Apoptosis Autophagy PARP Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields .
    Sweroside
  • HY-131592
    Tricetin
    1 Publications Verification

    		 Apoptosis Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway .
    Tricetin
  • HY-120371
    CPUY192018
    1 Publications Verification

    		 Keap1-Nrf2 Apoptosis Reactive Oxygen Species (ROS) NF-κB Inflammation/Immunology
    CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, with an IC50 of 0.63 µM. CPUY192018 exhibits anti-inflammatory and antioxidant activities. CPUY192018 can activate the Nrf2-dependent antioxidant pathway and inhibit the NF-κB-related inflammatory response. CPUY192018 can be used in the research of inflammation-related diseases .
    CPUY192018
  • HY-B0854
    Mancozeb

    		Environmental Pollutants Lactate Dehydrogenase Apoptosis Fungal Cytochrome P450 Keap1-Nrf2 Infection Metabolic Disease Cancer
    Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells .
    Mancozeb
  • HY-103435
    Vialinin A
    2 Publications Verification

    Terrestrin A

    		 Deubiquitinase TNF Receptor E1/E2/E3 Enzyme Keap1-Nrf2 Inflammation/Immunology Cancer
    Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke .
    Vialinin A
  • HY-173444
    HDAC11-IN-3

    		HDAC Transferrin Receptor Apoptosis Ferroptosis Cancer
    HDAC11-IN-3 (Compound A9) is a selective HDAC11 inhibitor (IC50: 4.1 nM). HDAC11-IN-3 has inhibitory effects on U937 and OCI-AML2 acute myeloid leukemia (AML) cell lines (IC50: 10 μM). HDAC11-IN-3 has significant anti-AML activity, inducing apoptosis, cell cycle arrest, and differentiation. HDAC11-IN-3 upregulates the iron transporters transferrin (TF) and transferrin receptor (TFRC), and activates the p62-Keap1-Nrf2-HMOX1 pathway, which together lead to increased intracellular iron levels and induce ferroptosis in AML cells. HDAC11-IN-3 can be used alone or in combination with Cytarabine (HY-13605) for AML research .
    HDAC11-IN-3
  • HY-141439
    TBE 31

    		Keap1-Nrf2 Quinone Reductase Glutathione S-transferase Apoptosis TNF Receptor Inflammation/Immunology Cancer
    TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .
    TBE 31
  • HY-178054
    LMDP10

    		Keap1-Nrf2 Drug Derivative Neurological Disease
    LMDP10 is an orally active 3-amino quinazoline derivative with Keap1-Nrf2 pathway activation activity. LMDP10 binds to Keap1 to inhibit Keap1-Nrf2 interaction, thereby activating the Nrf2 pathway. LMDP10 elevates Nrf2, SOD, and GSH levels, reduces MDA and TNF-α levels, attenuates neurodegeneration, and improves memory function in Alzheimer’s disease (AD) rats. LMDP10 can be used for the study of AD .
    LMDP10
  • HY-175548
    Nrf2 activator-21

    		Keap1-Nrf2 Apoptosis Caspase Neurological Disease
    Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury .
    Nrf2 activator-21
  • HY-174395
    CD-10

    		Keap1-Nrf2 Interleukin Related Heme Oxygenase (HO) Neurological Disease
    CD-10 is an orally active and BBB-penatrable Keap1-Nrf2 protein-protein interaction (PPI) inhibitor. CD-10 binds to Keap1 with a KD value of 193 nM. CD-10 exhibits potent anti-oxidative and anti-inflammatory effects through Keap1-Nrf2 pathway activation, evidenced by reduced levels of MDA, IL-4, IL-10 and increased expression of HO-1. CD-10 effectively alleviated anxiety and depressive behaviors and restored serum neurotransmitter levels by promoting Nrf2 nuclear translocation in the chronic unpredictable mild stress (CUMS) mouse model. CD-10 can be used for the study of depression.
    CD-10
  • HY-W701218
    Sulforaphane-d8

    		Reactive Oxygen Species (ROS) Cancer
    Sulforaphane-d8 is the deuterium labeled Sulforaphane (HY-13755). Sulforaphane is an orally active inducer of the Keap1/Nrf2/ARE pathway. Sulforaphane promotes the transcription of tumor-suppressing proteins and effectively inhibits the activity of HDACs. Through the activation of the Keap1/Nrf2/ARE pathway and further induction of HO-1 expression, Sulforaphane protects the heart. Sulforaphane suppresses high glucose-induced pancreatic cancer through AMPK-dependent signal transmission. Sulforaphane exhibits both anticancer and anti-inflammatory properties .
    Sulforaphane-d8
  • HY-W505984
    TPNA10168

    KM05073

    		 Keap1-Nrf2 Inflammation/Immunology
    TPNA10168 is an Nrf-2 activator that activates the Keap1-Nrf2-ARE pathway. TPNA10168 is neuroprotective against oxidative stress-induced damage. TPNA10168 significantly reduces the transcription of inflammatory genes, including TNF-α, IL-1β, IL-6, and iNOS. TPNA10168 can be used in research on anti-inflammatory and neurological diseases .
    TPNA10168
  • HY-175833
    NF-κB-IN-20

    		NF-κB Keap1-Nrf2 Heme Oxygenase (HO) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) SOD Inflammation/Immunology
    NF-κB-IN-20 is an orally active NF-κB inhibitor. NF-κB-IN-20 directly binds to the Keap1 protein, activating the Keap1/Nrf2/HO-1 antioxidant pathway, and simultaneously inhibiting the NF-κB inflammatory pathway, thereby synergistically reducing oxidative stress and inflammatory responses. NF-κB-IN-20 M11 inhibits the expression of IL-6, IL-1β, and TNF-α, significantly reduces the level of ROS, and restores the mitochondrial membrane potential. NF-κB-IN-20 can be used for the study of acute lung injury (ALI) .
    NF-κB-IN-20
  • HY-173181
    Anticonvulsant agent 10

    		Keap1-Nrf2 Neurological Disease
    Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a potent ED50 of 0.04 mmol/kg. By inhibiting Keap1-Nrf2 binding and activating the Nrf2/ARE pathway, Anticonvulsant agent 10 exerts anticonvulsant and neuroprotective effects, making it suitable for research in antiepileptic and neuroprotective studies .
    Anticonvulsant agent 10
  • HY-176146
    Keap1/Nrf2/ARE activator 1

    		Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    Keap1/Nrf2/ARE activator 1 (compound HT-3) is a Keap1/Nrf2/ARE pathway activator. Keap1/Nrf2/ARE activator 1 exhibits antioxidant activity and neuroprotective efficacy .
    Keap1/Nrf2/ARE activator 1
  • HY-181818
    4,5-Dehydro-6-oxoallosecurinine

    		Keap1-Nrf2 NO Synthase TNF Receptor Interleukin Related Neurological Disease Inflammation/Immunology
    4,5-Dehydro-6-oxoallosecurinine is a Keap1-Nrf2 pathway activator. 4,5-Dehydro-6-oxoallosecurinine promotes the nuclear translocation of Keap1-Nrf2, and induces the expression of antioxidant and cytoprotective genes. 4,5-Dehydro-6-oxoallosecurinine reduces the production of NO, and decreases the levels of iNOS, TNF-α, IL-6 and IL-1β in LPS-stimulated microglia. 4,5-Dehydro-6-oxoallosecurinine can be used for the research of neurodegenerative diseases .
    4,5-Dehydro-6-oxoallosecurinine
  • HY-N0806R
    Sweroside (Standard)

    		Reference Standards Keap1-Nrf2 AMPK Sirtuin NF-κB NOD-like Receptor (NLR) Pyroptosis Apoptosis Autophagy PARP Metabolic Disease
    Sweroside (Standard) is the analytical standard of Sweroside (HY-N0806). This product is intended for research and analytical applications. Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields .
    Sweroside (Standard)
  • HY-113298R
    Citraconic acid (Standard)

    Methylmaleic acid (Standard)

    		 Reference Standards NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Citraconic acid (Methylmaleic acid) (Standard) is the analytical standard of Citraconic acid (HY-113298). This product is intended for research and analytical applications. Citraconic acid is an orally active inhibitor targeting the NLRP3 inflammasome and Keap1-Nrf2 pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052) .
    Citraconic acid (Standard)
  • HY-168709
    Nrf2 activator 18

    		Keap1-Nrf2 Inflammation/Immunology
    Nrf2 activator 18 (Compound 11a) is an orally active activator for Keap1/Nrf2/HO-1 signaling pathway, that promotes the Nrf2 nuclear translocation, and enhances the antioxidant efficacy. Nrf2 activator 18 inhibits the release of IL-6 with an IC50 of 4.816 μM. Nrf2 activator 18 exhibits anti-inflammatory efficacy in mouse PM2.5-induced lung injury model .
    Nrf2 activator 18
  • HY-161643
    S21-1011

    		Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model .
    S21-1011
  • HY-N0147R
    Rutaecarpine (Standard)

    Rutecarpine (Standard)

    		 Reference Standards COX Keap1-Nrf2 Inflammation/Immunology Cancer
    Rutaecarpine (Standard) is the analytical standard of Rutaecarpine. This product is intended for research and analytical applications. Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine (Standard)
  • HY-175217
    Nrf2 activator-20

    		Keap1-Nrf2 Cardiovascular Disease Inflammation/Immunology
    Nrf2 activator-20 is a potent Nrf2 activator with anti-inflammatory and antioxidant activities. Nrf2 activator-20 activates the anti-inflammatory pathway by interfering with the Keap1-Nrf2 interaction and is beneficial in vivo. Nrf2 activator-20 can be used for the study of acute respiratory distress syndrome (ARDS) and ischemia-reperfusion injury .
    Nrf2 activator-20
  • HY-181887
    Nrf2 activator-23

    		Keap1-Nrf2 NF-κB p38 MAPK Metabolic Disease
    Nrf2 activator-23 is an orally active Keap1 binder and Nrf2 activator, with KD values of 28.68 nM and 54.55 nM for Keap1 and its Kelch domain, respectively. Nrf2 activator-23 disrupts the Keap1-Nrf2 interaction, reduces ubiquitination and degradation of Nrf2, and activates the Nrf2 signaling pathway. Nrf2 activator-23 inhibits RANKL-induced osteoclast formation, bone resorptive activity, ROS production, and activation of the MAPK and NF-κB signaling pathways, while downregulating the expression of osteoclast-specific genes and proteins. Nrf2 activator-23 attenuates bone loss and reduces osteoclast formation in vivo without affecting osteoblast differentiation and mineralization. Nrf2 activator-23 can be used for the research of osteoporosis .
    Nrf2 activator-23
  • HY-180155
    Keap1/Nrf2/ARE activator 2

    		Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase Neurological Disease
    Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease .
    Keap1/Nrf2/ARE activator 2
  • HY-181907
    NBE5

    		HyT Keap1-Nrf2 HSP Inflammation/Immunology
    NBE5 is an orally active hydrophobic tag-targeting (Hyt) degrader (HyTTD) that targets Keap1. NBE5 mimics protein misfolding and recruits the molecular chaperone Hsp90, while achieving targeted degradation of Keap1 through both the ubiquitin-proteasome system and the autophagy-lysosome system. Consequently, NBE5 relieves the inhibition of the transcription factor Nrf2 by Keap1, potently activates the Nrf2-mediated endogenous antioxidant pathway, and upregulates the expression of downstream antioxidant proteins such as HO-1 and GCLM. NBE5 effectively alleviates oxidative stress and inflammatory damage, and exhibits excellent in vivo activity in a mouse model of acute colitis induced by DSS (HY-116282C) .
    NBE5 consists of a hydrophobic tag (HY-W022007), a Keap1-Nrf2 ligand (HY-14909), and a linker (HY-W014831).
    NBE5
  • HY-N17603
    Ginnalin A

    Acertannin

    		 Keap1-Nrf2 p62 Heme Oxygenase (HO) Cancer
    Ginnalin A (Acertannin) is a Nrf2 activator. Ginnalin A shows antiproliferative activity against HCT116, SW480 and SW620 cells with IC50 values of 24.8, 22.0, and 39.7 μM, respectively. Ginnalin A can induce cancer cells S phase arrest. Ginnalin A can activate the p62-Keap1-Nrf2 signaling pathway, significantly upregulate the mRNA and protein expression of Nrf2, HO-1, and NQO1, and promote the transport of Nrf2 from the cytoplasm to the nucleus. Ginnalin A can be used for the research of colon cancer .
    Ginnalin A

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