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KEAP 1

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102

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-RS07230

    Small Interfering RNA (siRNA) Others

    KEAP1 Human Pre-designed siRNA Set A contains three designed siRNAs for KEAP1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

    KEAP1 Human Pre-designed siRNA Set A
    KEAP1 Human Pre-designed siRNA Set A
  • HY-151362
    Keap1-Nrf2-IN-14
    1 Publications Verification

    Keap1-Nrf2 Reactive Oxygen Species (ROS) 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-RS07231

    Small Interfering RNA (siRNA) Others

    Keap1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Keap1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Keap1 Mouse Pre-designed siRNA Set A
    Keap1 Mouse Pre-designed siRNA Set A
  • HY-RS07232

    Small Interfering RNA (siRNA) Others

    Keap1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Keap1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

    Keap1 Rat Pre-designed siRNA Set A
    Keap1 Rat Pre-designed siRNA Set A
  • HY-174287

    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-170301

    Quinone Reductase Keap1-Nrf2 Others
    Keap1-IN-1 (Compound 27) is the inhibitor for Keap1, that covalently modifys the Cys151 site in the BTB domain of KEAP1, and interfers with the interaction between Keap-Nrf. Keap1-IN-1 upregulates the mRNA expression of the antioxidant stress element (ARE)-dependent gene NQO1 with an EC50 of 160 nM. Keap1-IN-1 exhibits cytotoxicity in cell U2OS with an EC50 of 527 nM .
    Keap1-IN-1
  • HY-P5909

    Keap1-Nrf2 Cancer
    Keap1-Nrf2 probe is a Keap1-Nrf2 probe .
    Keap1-Nrf2 probe
  • 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-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-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-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-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-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-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-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-P5480

    Keap1-Nrf2 Others
    Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding activity)
    Keap1-Nrf2-IN-16
  • 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-168922

    Keap1-Nrf2 Reactive Oxygen Species (ROS) 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-172598

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-28 (SG16) is an orally active Keap1-Nrf2 inhibitor. Keap1-Nrf2-IN-28 shows antioxidant capability and induces the upregulation of Nrf2, HO-1, GCLM, and Akr1c1. Keap1-Nrf2-IN-28 attenuates APAP (HY-66005)-induced acute liver injury .
    Keap1-Nrf2-IN-28
  • 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 no cytotoxic activity in ARPE19 cells .
    Keap1-Nrf2-IN-9
  • 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
  • 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-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-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-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 (ROS) Quinone Reductase 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-173187

    Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-27 (compound 1C) is a inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) with KD2 value of 0.119 μM. Keap1-Nrf2-IN-27 suppresses the expression of pro-inflammatory cytokine TNF-α and IL-6 in the LPS-induced RAW264.7 cell model .
    Keap1-Nrf2-IN-27
  • 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-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-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-Nrf2-IN-15
  • HY-176146

    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-P5909F

    Keap1-Nrf2 Others
    FITC-labelled Keap1-Nrf2 probe is aFITC-labeled Keap1-Nrf2 probe (HY-P5909).
    FITC-labelled Keap1-Nrf2 probe
  • 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-149508

    Keap1-Nrf2 Reactive Oxygen Species (ROS) 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-173181

    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-111126
    K67
    1 Publications Verification

    p62 Keap1-Nrf2 Cancer
    K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocking the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2 .
    K67
  • HY-124941

    Keap1-Nrf2 Reactive Oxygen Species (ROS) Inflammation/Immunology
    7-Deacetylgedunin is an activator of Keap1/Nrf2/HO-1. 7-Deacetylgedunin alleviates mice mortality induced by LPS. 7-Deacetylgedunin inhibits Keap1 expression and suppresses macrophage proliferation. 7-Deacetylgedunin suppresses inflammation in vivo and in vitro .
    7-Deacetylgedunin
  • 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

    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-174395

    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-101140A

    Keap1-Nrf2 Metabolic Disease Inflammation/Immunology
    KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction .
    KI696 isomer
  • HY-13755
    Sulforaphane
    50+ Cited Publications

    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-110258B

    (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-171035

    Quinone Reductase Keap1-Nrf2 Aminotransferases (Transaminases) Metabolic Disease
    PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction. PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice .
    PRL-295
  • HY-W701218

    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-139620

    PROTACs Cancer
    MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
    MS83
  • 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-149010

    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-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

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