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NRF2

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337

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5

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Click Chemistry

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 .
    Nrf2 activator-2
  • 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-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 .
    Nrf2 degrader 1
  • 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-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-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-161992

    Keap1-Nrf2 Apoptosis Neurological Disease Inflammation/Immunology
    Nrf2 activator-11 (compound M11) is a Nrf2 activator with blood-brain permeability. Nrf2 activator-11 has anti-oxidation, anti-inflammation, anti-ferroptosis and anti-apoptosis. Nrf2 activator-11 can be used to study cerebral  ischemia-reperfusion (CI/R) injury models .
    Nrf2 activator-11
  • 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-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-P10530

    Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of Keap1 protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases .
    Nrf2 (69-84)
  • 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-124834

    Keap1-Nrf2 Apoptosis Cancer
    Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent inducer for antioxidant response element (ARE) (EC50 is 2.7 μM) and an activator for Nrf2. Nrf2 activator-10 modifies Keap1, blocks Cul3-Keap1 ubiquitin ligase complex, activates the transcription of Nrf2. Nrf2 activator-10 protects cells from H2O2-induced apoptosis.
    Nrf2 activator-10
  • HY-173307

    Reactive Oxygen Species Keap1-Nrf2 Apoptosis Cardiovascular Disease
    Nrf2 activator 19 is a BBB-penetrable NRF2/HO-1 activator. Nrf2 activator 19 exerts potent antioxidant and neuroprotective effects. Nrf2 activator 19 can also effectively reduce brain damage, reduce Reactive Oxygen Species (ROS) accumulation. Nrf2 activator 19 inhibits neuronal apoptosis. Nrf2 activator 19 promotes the recovery of neurological function and motor ability. Nrf2 activator 19 shows significant potential in ischemic stroke research .
    Nrf2 activator 19
  • 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-169315

    Keap1-Nrf2 Cancer
    Nrf2 activator 17 (compound 10) is an Nrf2 activator that inhibits the interaction between Keap1 and Nrf2 with an IC50 of < 0.1 pM. Additionally, Nrf2 activator 17 has an EC50 of < 10 μM in HepG2 cells .
    Nrf2 activator 17
  • HY-168709

    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-169201

    Keap1-Nrf2 Cancer
    Nrf2 activator-12 (compund 10v) potently activates Nrf2 (EC50=83.5 nM) and exhibits promising pharmacological properties, reversing disease progression and alleviating demyelination in an experimental autoimmune encephalomyelitis mouse model .
    Nrf2 activator-12
  • HY-RS16271

    Small Interfering RNA (siRNA) Keap1-Nrf2 Others
    Nrf-2 Mouse Pre-designed siRNA Set A includes three pairs of siRNA designed for different regions of the Nrf-2 (Mouse) gene, along with a negative control, a FAM-labeled negative control, and a positive control.
    Nrf-2 Mouse Pre-designed siRNA Set A
    Nrf-2 Mouse Pre-designed siRNA Set A
  • 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-101025
    Nrf2-IN-1
    5 Publications Verification

    Keap1-Nrf2 Cancer
    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) .
    Nrf2-IN-1
  • HY-149508

    Keap1-Nrf2 Reactive Oxygen Species Cancer
    Nrf2-IN-3 (Compound R16) is a small-molecule NRF2 inhibitor and increases reactive oxygen species (ROS) production. Nrf2-IN-3 selectively binds KEAP1 mutants and restores their NRF2-inhibitory function by repairing the disrupted KEAP1/NRF2 interactions, leading to proteasome-dependent NRF2 degradation in cells. Nrf2-IN-3 sensitizes KEAP1-mutated tumor cells to Cisplatin (HY-17394), Gefitinib (HY-50895), and KEAP1 G333C-mutated xenograft to Cisplatin .
    Nrf2-IN-3
  • 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-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-170867

    Keap1-Nrf2 Heme Oxygenase (HO) Reactive Oxygen Species Cardiovascular Disease
    Nrf2/HO-1 activator 3 (Compound C3a) is the activator for Nrf2 signaling pathway that promotes the Nrf2 translocation into nuclei and upregulates the expression of heme oxygenase-1 HO-1. Nrf2/HO-1 activator 3 inhibits the overespression of ROS and MDA in H2O2- or glucose-stimulated H9c2 cardiomyocytes, inhibits the cell viability and colony formation, thereby exhibiting antioxidant efficacy .
    Nrf2/HO-1 activator 3
  • 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 .
    Nrf2-ARE/hMAO-B/QR2 modulator 1
  • 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-Nrf2-IN-11
  • HY-145390A

    Keap1-Nrf2 Inflammation/Immunology
    (R,R)-Nrf2 activator-1 is the enantiomer of Nrf2 activator-1. 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 .
    (R,R)-Nrf2 activator-1
  • HY-159495

    Keap1-Nrf2 Metabolic Disease Cancer
    Keap1-Nrf2-IN-21 (compound 4d) is a glucose metabolism inhibitor with antitumor activity. Keap1-Nrf2-IN-21 inhibits glycolytic activity of cancer cells by targeting the glycolytic pathway, especially by affecting the Keap1-Nrf2 signaling pathway, thereby inhibiting tumor growth. Keap1-Nrf2-IN-21 exhibits cytotoxicity against the HEC1A cell line (IC50=2.60 μM) .
    Keap1-Nrf2-IN-21
  • 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-Nrf2-IN-9
  • HY-P5909

    Keap1-Nrf2 Cancer
    Keap1-Nrf2 probe is a Keap1-Nrf2 probe .
    Keap1-Nrf2 probe
  • 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-Nrf2-IN-14
  • HY-168526

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-24 (compound 57) is a potent Keap1-Nrf2 inhibitor with a Ki value of 13 nM. Keap1-Nrf2-IN-24 increases the protein expression of TRXR1 and NQO1. Keap1-Nrf2-IN-24 increases the AKR1B10 mRNA expression. Keap1-Nrf2-IN-24 shows good metabolic stability .
    Keap1-Nrf2-IN-24
  • HY-168161

    Keap1-Nrf2 Cancer
    Keap1-Nrf2-IN-23 (compound 56) is an inhibitor of the Keap1–Nrf2 PPI (IC50=16.0 nM). Keap1-Nrf2-IN-23 binds to Keap1 with a Kd value of 3.07 nM. Keap1-Nrf2-IN-23 has oral activity .
    Keap1-Nrf2-IN-23
  • 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-Nrf2-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-Nrf2-IN-7
  • 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-Nrf2-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-Nrf2-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-Nrf2-IN-12
  • HY-168922

    Keap1-Nrf2 Reactive Oxygen Species Interleukin Related Inflammation/Immunology
    Keap1-Nrf2-IN-25 (Compound 19) is a potent Keap1-Nrf2 inhibitor (IC50 of 0.55 μM) with Keap1 binding affinity (Kd of 0.50 μM). Keap1-Nrf2-IN-25 activates Nrf2, reduces ROS and pro-inflammatory cytokines (IL-1β, IL-6). Keap1-Nrf2-IN-25 exerts protective effects against DSS (HY-116282)-induced colitis .
    Keap1-Nrf2-IN-25
  • HY-162096

    Keap1-Nrf2 Cancer
    Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of Keap1-Nrf2 protein-protein interaction .
    Keap1-Nrf2-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-Nrf2-IN-3
  • 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/Nrf2 modulator 1
  • HY-P5909F

    Keap1-Nrf2 Others
    FITC-labelled Keap1-Nrf2 probe is aFITC-labeled Keap1-Nrf2 probe (HY-P5909).
    FITC-labelled Keap1-Nrf2 probe
  • 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-Nrf2-IN-4
  • HY-168065

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-22 (compound 19) is a Keap1-Nrf2 inhibitor, with a KD2 value of 42.2 nM for Keap1. Keap1-Nrf2-IN-22 can be used for the study of acute lung injury (ALI) and cerebral ischemia/reperfusion (I/R) injury .
    Keap1-Nrf2-IN-22
  • 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-Nrf2-IN-19
  • HY-147548

    Reactive Oxygen Species 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-Nrf2-IN-10
  • HY-170761

    Keap1-Nrf2 Cancer
    KEAP1-NRF2 PPI-IN-1 (compound 23) is an inhibitor targeting the KEAP1-NRF2 interaction. KEAP1-NRF2 PPI-IN-1 has IC50 values of 136 nM and 62 nM in the DNA damage assays of human TK6 and insect SF9 cell lines, respectively .
    KEAP1-NRF2 PPI-IN-1
  • 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-Nrf2-IN-18
  • 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-Nrf2-IN-13

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