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Pathways Recommended: Vitamin D Related/Nuclear Receptor
Results for "

Nrf2 nuclear translocation

" in MedChemExpress (MCE) Product Catalog:

29

Inhibitors & Agonists

11

Natural
Products

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-171705
    KMS99220

    		Keap1-Nrf2 Neurological Disease
    KMS99220 is an orally active Nrf2 inhibitory protein Keap-1 activator. KMS99220 promotes Nrf2 nuclear translocation, up-regulates the gene expression of antioxidant enzymes (such as heme oxygenase-1, etc.) and proteasome subunits, alleviates oxidative stress and protein aggregation damage. KMS99220 can be used in the research of Parkinson’s disease (PD) .
    KMS99220
  • HY-W009731
    Dibenzoylmethane

    		Keap1-Nrf2 Metabolic Disease Cancer
    Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2 .
    Dibenzoylmethane
  • HY-110258
    ML334
    5+ Cited Publications

    LH601A

    		 Quinone Reductase Keap1-Nrf2 Cancer
    ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    ML334
  • HY-121523
    MIND4-17

    		Keap1-Nrf2 Metabolic Disease
    MIND4-17 is a potent NRF2 activator that covalently modifies a C151 residue of Keap1. MIND4-17 disrupts Keap1-Nrf2 association, leading to Nrf2 protein stabilization and nuclear translocation. MIND4‐17 exerts potent antioxidant activity .
    MIND4-17
  • HY-110258B
    (R,S,R)-ML334

    (R,S,R)-LH601A

    		 Drug Isomer Cancer
    (R,S,R)-ML334 is the isomer of ML334 (HY-110258), and can be used as an experimental control. ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity .
    (R,S,R)-ML334
  • HY-162152
    biKEAP1

    		Keap1-Nrf2 Inflammation/Immunology
    biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models .
    biKEAP1
  • HY-147924
    Keap1-Nrf2-IN-11

    		Keap1-Nrf2 NO Synthase ROS Kinase Inflammation/Immunology
    Keap1-Nrf2-IN-11 (compound 6k) is a Keap1-Nrf2 inhibitor with KD2 value of 0.21 nM. Keap1-Nrf2-IN-11 inhibits the productions of ROS and NO and the expression of TNF-α. Keap1-Nrf2-IN-11 relieves inflammations by increasing the Nrf2 nuclear translocation. Keap1-Nrf2-IN-11 can be used for anti-inflammatory research .
    Keap1-Nrf2-IN-11
  • 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-W009731R
    Dibenzoylmethane (Standard)

    		Reference Standards Keap1-Nrf2 Metabolic Disease Cancer
    Dibenzoylmethane (Standard) is the analytical standard of Dibenzoylmethane. This product is intended for research and analytical applications. Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2 .
    Dibenzoylmethane (Standard)
  • HY-149246
    Aβ-IN-6

    		Amyloid-β Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    Aβ-IN-6 reduces pro-inflammatory cytokine release from microglia cells. Aβ-IN-6 significantly induces Nrf2 nuclear translocation and hamperes Aβ oligomers formation. Aβ-IN-6 exerts a consistent neuroprotective effect by modulating the redox-sensitive signalling pathways in vivo oxidative stress model. Aβ-IN-6 is an orally active and has antiinflammatory, Antioxidant and Anti-oligomeric activity. Aβ-IN-6 has the potential for Alzheimer's disease (AD) research .
    Aβ-IN-6
  • HY-N0290
    Mangiferin
    Maximum Cited Publications
    14 Publications Verification

    		 NF-κB Keap1-Nrf2 Apoptosis Cancer
    Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities .
    Mangiferin
  • HY-174287
    Keap1-IN-2

    		Keap1-Nrf2 Inflammation/Immunology
    Keap1-IN-2 (Compound 164) is a KEAP1 inhibitor (IC50: 2 nM). Keap1-IN-2 indirectly activates Nrf2 by inhibiting KEAP1, thereby enhancing the antioxidant capacity of cells. Keap1-IN-2 promotes the accumulation and nuclear translocation of Nrf2 by blocking KEAP1-mediated Nrf2 degradation. Keap1-IN-2 can be used to study diseases associated with oxidative stress, such as inflammatory bowel disease, Crohn's disease, and immune diseases such as ulcerative colitis .
    Keap1-IN-2
  • HY-N15190
    Sesaminol

    		Quinone Reductase Keap1-Nrf2 Reactive Oxygen Species (ROS) Neurological Disease
    Sesaminol is an orally active activator for Nrf2-ARE pathway, that promotes the the nuclear translocation of Nrf2 and enhances the NQO1 expression, thereby enhances the cell's defense against oxidative stress. Sesaminol inhibits 6-OHDA (HY-B1081)-induced ROS production and apoptosis in cell SH-SY5Y. Sesaminol exhibits neuroprotective efficacy against Rotenone (HY-B1756)-induced Parkinson's disease .
    Sesaminol
  • HY-100609
    4-P-PDOT
    5+ Cited Publications

    		 Melatonin Receptor Neurological Disease
    4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity) .
    4-P-PDOT
  • HY-149010
    NXPZ-2

    		Keap1-Nrf2 Neurological Disease
    NXPZ-2 is an orally active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with a Ki value of 95 nM, EC50 value of 120 and 170 nM. NXPZ-2 can dose-dependently ameliorate Aβ[1-42]-Induced cognitive dysfunction, improve brain tissue pathological changes in Alzheimer’s disease (AD) mouse by increasing neuron quantity and function. NXPZ-2 can inhibit oxidative stress by increasing Nrf2 expression levels and promoting its cytoplasm to nuclear translocation, which is helpful for Keap1-Nrf2 PPI inhibitors and AD associated disease research .
    NXPZ-2
  • 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-N0290R
    Mangiferin (Standard)

    		Reference Standards NF-κB Keap1-Nrf2 Apoptosis Cancer
    Mangiferin (Standard) is the analytical standard of Mangiferin. This product is intended for research and analytical applications. Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50. Mangiferin exhibits antioxidant, antidiabetic, antihyperuricemic, antiviral, anticancer and antiinflammatory activities .
    Mangiferin (Standard)
  • HY-N0806
    Sweroside
    2 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-100609R
    4-P-PDOT (Standard)

    		Reference Standards Melatonin Receptor Neurological Disease
    4-P-PDOT (Standard) is the analytical standard of 4-P-PDOT. This product is intended for research and analytical applications. 4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity) .
    4-P-PDOT (Standard)
  • HY-30267
    4-Hydroxyphenyl acetate
    2 Publications Verification

    4-HPA; 4-Acetoxyphenol

    		 Quinone Reductase Endogenous Metabolite Others
    4-Hydroxyphenyl acetate (4-HPA) is a natural antioxidant and protects cells from oxidative stress-induced necrosis. 4-Hydroxyphenyl acetate blocks the increase of cellular ROS induced by oxidative stress, and up-regulates NQO1 and HO-1 genes by stabilizing and inducing the nuclear translocation of NRF2 transcription factor .
    4-Hydroxyphenyl acetate
  • HY-N1902R
    4-Hydroxyphenylacetic acid (Standard)

    		Reference Standards Keap1-Nrf2 Endogenous Metabolite Metabolic Disease
    4-Hydroxyphenylacetic acid (Standard) is the analytical standard of 4-Hydroxyphenylacetic acid. This product is intended for research and analytical applications. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2 . IC50 & Target:Nrf2 In Vivo: 4-Hydroxyphenylacetic acid (6, 12, or 25 mg/kg) increases Nrf2 translocation to the nucleus and enhances the activity of phase II and antioxidant enzymes. The protein levels of nuclear Nrf2 are increased by 170% and 230% in pre-treated 12 and 25 mg/kg 4-Hydroxyphenylacetic acid groups, respectively, compared with the control group.The 4-Hydroxyphenylacetic acid pretreatment at a final dose of 25 mg/kg markedly and selectively up-regulated the target genes of phase II enzymes and resulted in higher up-regulation than that of the control group by 270%, 400%, and 500% or UGT1A1, UGT1A9, and SULT2A1, respectively. 4-Hydroxyphenylacetic acid also suppresses the expression of CYP2E1 .
    4-Hydroxyphenylacetic acid (Standard)
  • 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-B0916
    Propoxur

    		Insecticide Cholinesterase (ChE) MMP Reactive Oxygen Species (ROS) ERK Keap1-Nrf2 Infection Neurological Disease Cancer
    Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
    Propoxur
  • HY-N9602
    6,7,4'-Trihydroxyflavanone

    		Others Inflammation/Immunology
    6,7,4'-Trihydroxyflavanone is a compound with multiple pharmacological activities, including anti-rheumatic, anti-ischemic, anti-inflammatory, anti-osteoclastogenic and protective T-cells from METH-induced deactivation. 6,7,4'-Trihydroxyflavanone has shown potential protective effects in neurotoxicity studies and can be used to inhibit patients with neurodegenerative diseases caused by METH. 6,7,4'-Trihydroxyflavanone inhibits METH-induced neurotoxicity by upregulating the Nrf2/HO-1 and PI3K/Akt/mTOR signaling pathways. 6,7,4'-Trihydroxyflavanone can also induce Nrf2 nuclear translocation and HO-1 expression, further enhancing its protective effect on neuronal cells .
    6,7,4'-Trihydroxyflavanone
  • HY-30267R
    4-Hydroxyphenyl acetate (Standard)

    		Endogenous Metabolite Others
    4-Hydroxyphenyl acetate (Standard) is the analytical standard of 4-Hydroxyphenyl acetate. This product is intended for research and analytical applications. 4-Hydroxyphenyl acetate (4-HPA) is a natural antioxidant and protects cells from oxidative stress-induced necrosis. 4-Hydroxyphenyl acetate blocks the increase of cellular ROS induced by oxidative stress, and up-regulates NQO1 and HO-1 genes by stabilizing and inducing the nuclear translocation of NRF2 transcription factor .
    4-Hydroxyphenyl acetate (Standard)
  • HY-143243
    Antioxidant agent-5

    		Apoptosis NF-κB Keap1-Nrf2 Reactive Oxygen Species (ROS) Cardiovascular Disease
    Antioxidant agent-5 (compound D-6) is a potent antioxidant agent. Antioxidant agent-5 can inhibit oxLDL (oxidized low-density lipoprotein)-induced apoptosis and the expression of ICAM-1 and VCAM-1 in VECs. Antioxidant agent-5 suppresses oxLDL-induced increase of ROS level and nuclear translocation of NF-κB. Antioxidant agent-5 protects against oxLDL-induced endothelial injury by activating Nrf2/HO-1 anti-oxidation pathway .
    Antioxidant agent-5
  • HY-B0916S
    Propoxur-d3

    		Isotope-Labeled Compounds Insecticide Cholinesterase (ChE) MMP Reactive Oxygen Species (ROS) ERK Keap1-Nrf2 Infection Neurological Disease Cancer
    Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
    Propoxur-d3
  • HY-B0916R
    Propoxur (Standard)

    		Reference Standards MMP Insecticide Cholinesterase (ChE) Reactive Oxygen Species (ROS) ERK Keap1-Nrf2 Infection Neurological Disease Cancer
    Propoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
    Propoxur (Standard)
  • HY-159152
    PQM-164

    		α-synuclein Neurological Disease
    PQM-164 (Compound 3e) has antioxidant activity (IC50: 0.93 μM for DPPH radical). PQM-164 shows anti-inflammatory activity against 6-OHDA (HY-B1081A)-induced neuronal damage in activated microglial cells. PQM-164 decreases the accumulation of α-synuclein. PQM-164 promotes nuclear translocation of Nrf2 and its transcriptional activity. PQM-164 can be used for research of Parkinson’s disease .
    PQM-164

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