1. Search Result
Search Result
Results for "

Keap-1

" in MedChemExpress (MCE) Product Catalog:

102

Inhibitors & Agonists

3

Screening Libraries

8

Peptides

17

Natural
Products

5

Recombinant Proteins

5

Isotope-Labeled Compounds

4

Antibodies

1

Click Chemistry

3

Oligonucleotides

Targets Recommended:
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 [1].
    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 [1].
    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 [1].
    Keap1-IN-1
  • HY-P5909

    Keap1-Nrf2 Cancer
    Keap1-Nrf2 probe is a Keap1-Nrf2 probe [1].
    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 [1].
    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 [1].
    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 [1].
    Keap1-Nrf2-IN-24
  • 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 [1].
    Keap1-Nrf2-IN-22
  • 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 [1].
    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 [1].
    Keap1-Nrf2-IN-7
  • HY-P5480

    Keap1-Nrf2 Others
    Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding activity)
    Keap1-Nrf2-IN-16
  • 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 [1].
    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 [1].
    Keap1-Nrf2-IN-12
  • HY-162096

    Keap1-Nrf2 Cancer
    Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of Keap1-Nrf2 protein-protein interaction [1].
    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 [1].
    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 [1].
    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 [1].
    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 [1].
    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 [1].
    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 [1].
    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) [1].
    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 [1].
    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 [1].
    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 [1].
    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) [1].
    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 [1].
    KEAP1-NRF2 PPI-IN-1
  • 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 [1].
    Keap1/Nrf2/ARE activator 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 [1].
    Keap1-Nrf2-IN-15
  • HY-P5909F

    Keap1-Nrf2 Others
    FITC-labelled Keap1-Nrf2 probe is aFITC-labeled Keap1-Nrf2 probe (HY-P5909).
    FITC-labelled Keap1-Nrf2 probe
  • HY-171705

    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) [1].
    KMS99220
  • 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 [1].
    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 [1].
    Nrf2-IN-3
  • 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 [1] .
    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 [1].
    7-Deacetylgedunin
  • 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 [1].
    Anticonvulsant agent 10
  • 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 [1] .
    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 [1] .
    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 [1].
    KI696 isomer
  • 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 [1] .
    (R,S,R)-ML334
  • 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 [1] .
    Sulforaphane
  • HY-139620

    PROTACs Cancer
    MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
    MS83
  • 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 [1].
    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 [1] .
    Sulforaphane-d8
  • 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-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 [1].
    biKEAP1

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

 

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

 

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: