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NRF2 activation

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106

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2

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4

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11

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-115849

    Keap1-Nrf2 Neurological Disease
    Nrf2-Activator-12G (compd 12g) is an activator of Nrf2. Nrf2-Activator-12G induces the expression of nrf2-dependentantioxidant enzymes at both mRNA and protein levels in DAergic neuronal cell. Nrf2-Activator-12G can used in study Parkinson’s Disease .
    Nrf2-Activator-12G
  • HY-P1328
    TAT-14
    1 Publications Verification

    Keap1-Nrf2 Others
    TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1 .
    TAT-14
  • HY-148480

    Keap1-Nrf2 Cardiovascular Disease
    Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4) .
    Nrf2 activator-6
  • HY-P1328A

    Keap1-Nrf2 Others
    TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1 .
    TAT-14 TFA
  • HY-145390

    Keap1-Nrf2 Inflammation/Immunology
    Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the research of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1) .
    Nrf2 activator-1
  • HY-156081

    Keap1-Nrf2 Apoptosis Metabolic Disease
    Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis .
    Nrf2 activator-9
  • HY-163027

    Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    R079 (compound 17) is a selective, orally active Nrf2 activator. R079 increases Nrf2 translocation activity (EC50 = 32.41 μM). R079 can neutralize excess levels of reactive oxygen species through activating Nrf2. R079 has anti-inflammatory properties and can be used in multiple sclerosis research .
    R079
  • HY-162152

    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-145879

    Keap1-Nrf2 Cancer
    Nrf2 activator-2 (compound O15), a Osthole derivative, is a potent Nrf2 agonist with an EC50 of 2.9 μM in 293 T cells. Nrf2 activator-2 effectively inhibits the interaction between Keap1 and Nrf2, thus showing the activation effect on Nrf2. Nrf2 activator-2 shows a marked decrease in the level of ubiquitinated Nrf2 in cells .
    Nrf2 activator-2
  • HY-149244

    Keap1-Nrf2 Others
    Nrf2 activator-7 (Compound 12b) is a potent Nrf2 activator and significantly activates the Nrf2 signaling pathway.
    Nrf2 activator-7
  • HY-143333

    Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    Nrf2 activator-3 is a potent Nrf2 activator. Nrf2 activator-3 is used for cerebral ischemic injury research .
    Nrf2 activator-3
  • HY-19734
    NK-252
    5+ Cited Publications

    Keap1-Nrf2 Cancer
    NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
    NK-252
  • HY-151430

    Keap1-Nrf2 ERK Akt JNK Reactive Oxygen Species Neurological Disease
    Nrf2/HO-1 activator 1 (Compound 24) is a potent Nrf2/HO-1 activator, neuroprotective agent. Nrf2/HO-1 activator 1 shows neuroprotective and antioxidant activities. Nrf2/HO-1 activator 1 can be used in Parkinson's disease (PD) research .
    Nrf2/HO-1 activator 1
  • HY-122550

    Keap1-Nrf2 Topoisomerase Apoptosis Cancer
    Artemisitene, a natural derivative of Artemisinin, is a Nrf2 activator with antioxidant and anticancer activities. Artemisitene activates Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability .
    Artemisitene
  • HY-146086

    Keap1-Nrf2 Reactive Oxygen Species Neurological Disease Inflammation/Immunology
    Nrf2 activator-4 (Compound 20a) is a highly potent, orally active Nrf2 activator with an EC50 of 0.63 µM. Nrf2 activator-4 suppresses reactive oxygen species against oxidative stress in microglia. Nrf2 activator-4 effectively recovers the learning and memory impairment in a scopolamine-induced mouse model .
    Nrf2 activator-4
  • HY-151431

    Keap1-Nrf2 Reactive Oxygen Species ERK Akt JNK Neurological Disease
    Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD) .
    Nrf2/HO-1 activator 2
  • HY-155572

    Keap1-Nrf2 Inflammation/Immunology
    Nrf2 activator-8 (compound 10e) is a Nrf2 activator (EC50=37.9 nM). Nrf2 activator-8 exhibits remarkable antioxidant and anti-inflammatory effects in BV-2 microglial cells. Nrf2 activator-8 can significantly restore spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation .
    Nrf2 activator-8
  • HY-156065

    Keap1-Nrf2 Metabolic Disease
    S217879 is a highly potent and selective NRF2 activator. S217879 disrupts the KEAP1-NRF2 interaction leading to robust NRF2 pathway activation. S217879 can be used for non-alcoholic steatohepatitis (NASH) research .
    S217879
  • HY-146168

    Keap1-Nrf2 Inflammation/Immunology
    Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities .
    Nrf2 activator-5
  • HY-110258
    ML334
    5 Publications Verification

    LH601A

    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-144634

    Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD) .
    DDO-7263
  • HY-121523

    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-W009731

    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-100489
    TBHQ
    65+ Cited Publications

    tert-Butylhydroquinone

    Keap1-Nrf2 ERK Autophagy Apoptosis Ferroptosis Cancer
    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2 . TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma .
    TBHQ
  • HY-110275

    Keap1-Nrf2 Others
    RA839 is a noncovalent small molecule binder to Keap1 with a Kd of ∼6 μM and selective activator of Nrf2 signaling. RA839 prevents the induction of both inducible nitric-oxide synthase expression and nitric oxide release in response to lipopolysaccharides in macrophages. RA839 is a selective inhibitor of the Keap1/Nrf2 interaction and a useful tool compound to study the biology of Nrf2 .
    RA839
  • HY-12213
    CDDO-EA
    2 Publications Verification

    CDDO ethyl amide; TP319; RTA 405

    Keap1-Nrf2 Cancer
    CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
    CDDO-EA
  • HY-131592

    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-110258B

    (R,S,R)-LH601A

    Others 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-W505984

    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-101371

    Keap1-Nrf2 Cancer
    Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
    Hesperin
  • HY-N0509
    Astilbin
    2 Publications Verification

    Keap1-Nrf2 TNF Receptor NF-κB Inflammation/Immunology Cancer
    Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
    Astilbin
  • HY-100489R

    tert-Butylhydroquinone (Standard)

    Keap1-Nrf2 ERK Autophagy Apoptosis Ferroptosis Cancer
    TBHQ (Standard) is the analytical standard of TBHQ. This product is intended for research and analytical applications. TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2 . TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma .
    TBHQ (Standard)
  • HY-134205A
    CBR-470-1
    1 Publications Verification

    Keap1-Nrf2 Neurological Disease Metabolic Disease
    CBR-470-1 is an inhibitor of the glycolytic enzyme phosphoglycerate kinase 1 (PGK1). CBR-470-1 is also a non-covalent Nrf2 activator. CBR-470-1 protects SH-SY5Y neuronal cells against MPP +-induced cytotoxicity through activation of the Keap1-Nrf2 cascade .
    CBR-470-1
  • HY-N12486

    Keap1-Nrf2 ATP Synthase Metabolic Disease
    Isofalcarintriol is a NRF2 activator and selective inhibitor of the mitochondrial ATP synthase. Isofalcarintriol can be used for aging study .
    Isofalcarintriol
  • HY-N0643
    Carnosol
    5+ Cited Publications

    Ribosomal S6 Kinase (RSK) Keap1-Nrf2 Endogenous Metabolite Cancer
    Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM . Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1) .
    Carnosol
  • HY-14645A
    (+)-DHMEQ
    2 Publications Verification

    (1R,2R,6R)-Dehydroxymethylepoxyquinomicin; (1R,2R,6R)-DHMEQ

    Keap1-Nrf2 Inflammation/Immunology
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
    (+)-DHMEQ
  • HY-N1244

    Sarmentosine; Sarmentosine (glycoside)

    Keap1-Nrf2 mTOR Apoptosis Cancer
    Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells .
    Sarmentosin
  • HY-15725
    CDDO-Im
    5+ Cited Publications

    RTA-403; TP-235; CDDO-Imidazolide

    Keap1-Nrf2 PPAR Ferroptosis Cancer
    CDDO-Im (RTA-403) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ .
    CDDO-Im
  • HY-14909
    Bardoxolone
    10+ Cited Publications

    CDDO; RTA 401

    Keap1-Nrf2 Necroptosis Metabolic Disease
    Bardoxolone (CDDO) is a novel nuclear regulatory factor (Nrf-2) activator for the study of chronic kidney disease. Bardoxolone is a potent necroptosis inhibitor that inhibits Z-VAD-FMK-induced necroptosis .
    Bardoxolone
  • HY-N3260

    Reactive Oxygen Species Keap1-Nrf2 PI3K Inflammation/Immunology
    Methyllucidone is a neuroprotective agent and an antioxidant that can be isolated from Lindera erythrocarpa Makino. Methyllucidone inhibits the ROS production, and activates antioxidant signaling pathways that include Nrf-2 and PI3K .
    Methyllucidone
  • HY-N0892
    AKBA
    1 Publications Verification

    Acetyl-11-keto-β-boswellic acid

    HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species Endogenous Metabolite Cancer
    AKBA (Acetyl-11-keto-β-boswellic acid) is an active triterpenoid compound from the extract of Boswellia serrate and a novel Nrf2 activator.
    AKBA
  • HY-N0606
    Ginsenoside Rh3
    1 Publications Verification

    Keap1-Nrf2 Inflammation/Immunology
    Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.
    Ginsenoside Rh3
  • HY-112675
    4-Octyl itaconate
    40+ Cited Publications

    Keap1-Nrf2 Inflammation/Immunology
    4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1 .
    4-Octyl itaconate
  • HY-N0826
    Corynoline
    2 Publications Verification

    Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Corynoline is a reversible and noncompetitive acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM . Corynoline exhibits anti-inflammatory activity by activating Nrf2 .
    Corynoline
  • HY-112671

    RTA dh404

    Keap1-Nrf2 NF-κB Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
    CDDO-dhTFEA
  • HY-134001

    Keap1-Nrf2 Metabolic Disease
    CBR-470-2, a glycine-substituted analog, can activate NRF2 signaling. CBR-470-2 can be used for the research of modulation glycolysis .
    CBR-470-2
  • HY-12212
    Omaveloxolone
    15+ Cited Publications

    RTA 408

    Keap1-Nrf2 STING Apoptosis Inflammation/Immunology Cancer
    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
    Omaveloxolone
  • HY-13755
    Sulforaphane
    30+ Cited Publications

    HDAC Keap1-Nrf2 Apoptosis Bcl-2 Family Caspase Reactive Oxygen Species 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-13324
    Bardoxolone methyl
    20+ Cited Publications

    RTA 402; NSC 713200; CDDO Methyl ester

    Keap1-Nrf2 Autophagy Apoptosis Ferroptosis Cancer
    Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
    Bardoxolone methyl
  • HY-17376
    Ezetimibe
    5+ Cited Publications

    SCH 58235

    Keap1-Nrf2 Autophagy Cardiovascular Disease Cancer
    Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
    Ezetimibe

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