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NRF-2

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • 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 .
    <em>Nrf2</em> activator-<em>2</em>
  • 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 .
    <em>Nrf2</em> activator-4
  • HY-149244

    Keap1-Nrf2 Others
    Nrf2 activator-7 (Compound 12b) is a potent Nrf2 activator and significantly activates the Nrf2 signaling pathway.
    <em>Nrf2</em> activator-7
  • 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) .
    <em>Nrf2</em> activator-6
  • 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 .
    <em>Nrf2</em> activator-3
  • 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 .
    <em>Nrf2</em> activator-8
  • 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 .
    <em>Nrf2</em> activator-5
  • 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 .
    <em>Nrf2</em> activator-9
  • 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) .
    <em>Nrf2</em> activator-1
  • HY-162307

    PROTACs Keap1-Nrf2 Cancer
    Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with anticancer effects. Nrf2 degrader 1 inhibits cancer cells growth for A549 and LK-2 cells with IC50 values of 100 nM and 40 nM, respectively .
    <em>Nrf2</em> degrader 1
  • HY-149508

    Keap1-Nrf2 Cancer
    Nrf2-IN-3 (Compound R16) is a Nrf2 inhibitor. Nrf2-IN-3 binds KEAP1 mutants (G333C mKEAP1) and repairs the disrupted KEAP1/NRF2 interactions. Nrf2-IN-3 sensitizes KEAP1-mutated cancer cells to Cisplatin (HY-17394) and Gefitinib (HY-50895) by repairing the mKEAP1/NRF2 complex .
    <em>Nrf2</em>-IN-3
  • HY-101025
    Nrf2-IN-1
    2 Publications Verification

    Nrf2-IN-1 is an inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2). Nrf2-IN-1 is developed for the research of acute myeloid leukemia (AML) .
    <em>Nrf2</em>-IN-1
  • 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 .
    <em>Nrf2</em>-Activator-12G
  • 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 .
    <em>Nrf2</em>/HO-1 activator 1
  • 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) .
    <em>Nrf2</em>/HO-1 activator <em>2</em>
  • HY-144635

    Monoamine Oxidase Keap1-Nrf2 Reactive Oxygen Species Neurological Disease
    Nrf2-ARE/hMAO-B/QR2 modulator 1 is a Resveratrol-based multitarget-directed ligands with IC50s of 8.05, 9.83 and 0.57 μM for hMAO-B, NRF2 and QR2. Nrf2-ARE/hMAO-B/QR2 modulator 1 has neuroprotection, decreasing ROS production in okadaic acid-treated mice hippocampal slices .
    <em>Nrf2</em>-ARE/hMAO-B/QR<em>2</em> modulator 1
  • HY-P5909

    Keap1-Nrf2 Cancer
    Keap1-Nrf2 probe is a Keap1-Nrf2 probe .
    Keap1-<em>Nrf2</em> probe
  • HY-147924

    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-<em>Nrf2</em>-IN-11
  • HY-151362

    Keap1-Nrf2 Reactive Oxygen Species Inflammation/Immunology
    Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation .
    Keap1-<em>Nrf2</em>-IN-14
  • HY-143893

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-6 (compound 64) is a potent and selective Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 41 nM, Kd of 68 nM .
    Keap1-<em>Nrf2</em>-IN-6
  • HY-146577

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-7 (compound 7v) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 0.45 µM .
    Keap1-<em>Nrf2</em>-IN-7
  • HY-147517

    Keap1-Nrf2 Neurological Disease Inflammation/Immunology
    Keap1-Nrf2-IN-9 (compound 11) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 0.575 µM. Keap1-Nrf2-IN-9 increases the expression of Nrf2 target genes including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and glutamate-cysteine ligase catalytic (Gclc) and modulatory (Gclm) subunits. Keap1-Nrf2-IN-9 shows not cytotoxic activity in ARPE19 cells .
    Keap1-<em>Nrf2</em>-IN-9
  • HY-146578

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-8 (compound 12d) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with IC50s of 64.5 nM and 14.2 nM for FP and TR-FRET assays, respectively. Keap1-Nrf2-IN-8 significantly increases the mRNA levels of Nrf2 downstream genes, GSTM3, HMOX2 and NQO1 .
    Keap1-<em>Nrf2</em>-IN-8
  • HY-143892

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-5 (compound 1) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 4.1 µM, Kd of 3.7 µM .
    Keap1-<em>Nrf2</em>-IN-5
  • HY-150578

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-12 is a potent Keap1-Nrf2 inhibitor with an IC50 value of 2.30 µM. Keap1-Nrf2-IN-12 shows metabolic stability in human liver microsomes .
    Keap1-<em>Nrf2</em>-IN-12
  • HY-162096

    Keap1-Nrf2 Cancer
    Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of Keap1-Nrf2 protein-protein interaction .
    Keap1-<em>Nrf2</em>-IN-17
  • HY-139862

    Keap1-Nrf2 Others
    Keap1-Nrf2-IN-3 is a KEAP1:NRF2 protein−protein interaction inhibitor, and with a Kd value of 2.5 nM for KEAP1 protein.
    Keap1-<em>Nrf2</em>-IN-3
  • HY-144099

    E1/E2/E3 Enzyme Apoptosis Cancer
    Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity .
    Keap1-<em>Nrf2</em>-IN-4
  • HY-P5909F

    Keap1-Nrf2 Others
    FITC-labelled Keap1-Nrf2 probe is aFITC-labeled Keap1-Nrf2 probe (HY-P5909).
    FITC-labelled Keap1-<em>Nrf2</em> probe
  • HY-157929

    Keap1-Nrf2 Inflammation/Immunology Cancer
    Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs .
    Keap1-<em>Nrf2</em>-IN-19
  • HY-147548

    Others Others
    Keap1-Nrf2-IN-10 (compound 15) is a potent NQO1 inducer. Keap1-Nrf2-IN-10 inhibits oxidative stress by decreasing the levels of MDA, ROS, NQO1 in the liver for gamma-irradiated mice. Keap1-Nrf2-IN-10 improves the survival of gamma-irradiated mice .
    Keap1-<em>Nrf2</em>-IN-10
  • HY-157928

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
    Keap1-<em>Nrf2</em>-IN-18
  • HY-152037

    Cholinesterase (ChE) Keap1-Nrf2 Neurological Disease
    AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease .
    AChE/<em>Nrf2</em> modulator 1
  • HY-150579

    Keap1-Nrf2 Inflammation/Immunology Cancer
    Keap1-Nrf2-IN-13 is a Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with an IC50 value of 0.15 μM. Keap1-Nrf2-IN-13 has strong binding affinities to the Keap1 protein by forming hydrogen bond with the key polar residues (Asn414, Arg415, Arg483, Gln530). Keap1-Nrf2-IN-13 can be used in the research of oxidative stress-related and inflammatory diseases, including pulmonary fibrosis, chronic obstructive pulmonary disorder (COPD) and cancers .
    Keap1-<em>Nrf2</em>-IN-13
  • HY-149245

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-15 (Compound 24a) is a potent Keap1-Nrf2 protein-protein interaction inhibitor with IC50s of 77 nM and 2.5 nM in FP assay and TR-FRET assay, respectively .
    Keap1-<em>Nrf2</em>-IN-15
  • HY-P5480

    Keap1-Nrf2 Others
    Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding activity)
    Keap1-<em>Nrf2</em>-IN-16
  • 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-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 [2].
    Artemisitene
  • 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-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-101140
    KI696
    10+ Cited Publications

    Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction .
    KI696
  • 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-120371

    Others Inflammation/Immunology
    CPUY192018 is a potent Keap1-Nrf2-ARE inhibitor with an IC50 of 0.63 µM. CPUY192018 exhibits induction of Nrf2-dependent gene NQO1 at 100 µM .
    CPUY192018
  • 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 [2].
    ML334
  • HY-113848

    Keap1-Nrf2 Cancer
    AEM1 is a Nrf2 inhibitor . AEM1 reduces the expressions of Nrf2-dependent genes in A549 cells and inhibits the growth of A549 cells in vitro and in vivo [2].
    AEM1
  • 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 [2].
    MIND4-17
  • 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-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) [2].
    DDO-7263
  • 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-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

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