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keap1

" in MedChemExpress (MCE) Product Catalog:

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-112675
    4-Octyl itaconate
    85+ Cited Publications

    4-OI

    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 [1].
    4-Octyl itaconate
  • HY-13755
    Sulforaphane
    65+ 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-101140
    KI696
    15+ 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-159641

    BAY-3605349

    Molecular Glues Keap1-Nrf2 Metabolic Disease Inflammation/Immunology Cancer
    VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors [1] .
    VVD-130037
  • HY-N0147
    Rutaecarpine
    5+ Cited Publications

    Rutecarpine

    COX Keap1-Nrf2 Neurological Disease Inflammation/Immunology Cancer
    Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor of COX-2 with an IC50 value of 0.28 μM. Rutaecarpine can target and activate the NRF2/HO-1 pathway to reduce craniofacial injury. Rutaecarpine sttenuates oxidative stress-induced traumatic brain injury (TBI) and reduces secondary injury via the PGK1/KEAP1/NRF2 signaling pathway. Rutaecarpine can cross the blood-brain barrier (BBB).
    Rutaecarpine
  • HY-113298
    Citraconic acid
    4 Publications Verification

    Methylmaleic acid

    NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Citraconic acid (Methylmaleic acid) is an orally active inhibitor targeting the NLRP3 inflammasome and Keap1-Nrf2 pathway. Citraconic acid reduces reactive oxygen species (ROS) generation by inhibiting succinate dehydrogenase (SDH) activity. Citraconic acid also modifies the conformation of Keap1 protein, relieves its inhibition of Nrf2, promotes antioxidant gene expression, and inhibits NLRP3 activation and the release of pro-inflammatory factors such as IL-1β and IL-18. Citraconic acid has anti-inflammatory and antioxidant activities, can reduce oxidative stress and cell pyroptosis, improve tissue damage, and can be used for the research of inflammation-related diseases such as acute renal ischemia-reperfusion injury. Citraconic acid is an isomer of Itaconic acid (HY-Y052) [1] .
    Citraconic acid
  • 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-110258
    ML334
    10+ 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-N0806
    Sweroside
    3 Publications Verification

    Keap1-Nrf2 AMPK Sirtuin NF-κB NOD-like Receptor (NLR) Pyroptosis Apoptosis Autophagy PARP Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
    Sweroside is an iridoid glycoside that targets multiple targets, including the Keap1/Nrf2 axis, NLRP3 inflammasome, SIRT1, NF-κB, AMPK/mTOR pathway, and caspase family. Sweroside promotes Nrf2 nuclear translocation by competitively binding to Keap1. Sweroside also inhibits oxidative stress and NLRP3-mediated pyroptosis by activating Nrf2, inhibits NF-κB inflammatory pathway by activating SIRT1, and promotes autophagy and induces caspase-dependent apoptosis via the AMPK/mTOR pathway. Sweroside has antioxidant, anti-inflammatory, anti-apoptotic, and lipid metabolism regulating activities, and can be used in the research of myocardial ischemia-reperfusion injury, leukemia, acute lung injury, non-alcoholic fatty liver disease, and other fields [1] .
    Sweroside
  • HY-110275

    Keap1-Nrf2 NO Synthase Infection Inflammation/Immunology
    RA839 is a selective Nrf2/ARE pathway agonist and non-covalent small molecule binder of Keap1 (Kd is approximately 6 μM). RA839 prevents inducible nitric oxide synthase expression and nitric oxide release. RA839 exerts anti-rotaviral and anti-inflammatory effects [1] .
    RA839
  • HY-113162
    Bovinic acid
    1 Publications Verification

    Keap1-Nrf2 Ferroptosis Reactive Oxygen Species (ROS) SOD Metabolic Disease Cancer
    Bovinic acid is an orally active anti-inflammatory agent. Bovinic acid inhibits oxidative stress and ferroptosis by regulating the Keap1-Nrf2 signaling pathway. Bovinic acid exerts hepatoprotective effects against alcohol-associated liver disease. Bovinic acid can be used for the research of alcohol-associated liver disease [1].
    Bovinic acid
  • HY-W009731

    Environmental Pollutants 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 [1].
    Dibenzoylmethane
  • 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-131592
    Tricetin
    1 Publications Verification

    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 [1].
    Tricetin
  • 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-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-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 [1].
    Nrf2 activator-2
  • 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-120371
    CPUY192018
    1 Publications Verification

    Keap1-Nrf2 Apoptosis Reactive Oxygen Species (ROS) NF-κB Inflammation/Immunology
    CPUY192018 is a potent inhibitor of the Keap1-Nrf2 protein-protein interaction, with an IC50 of 0.63 µM. CPUY192018 exhibits anti-inflammatory and antioxidant activities. CPUY192018 can activate the Nrf2-dependent antioxidant pathway and inhibit the NF-κB-related inflammatory response. CPUY192018 can be used in the research of inflammation-related diseases [1] .
    CPUY192018
  • HY-B0854

    Environmental Pollutants Lactate Dehydrogenase Apoptosis Fungal Cytochrome P450 Keap1-Nrf2 Infection Metabolic Disease Cancer
    Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells [1] .
    Mancozeb
  • 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-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 [1].
    NXPZ-2
  • HY-103435
    Vialinin A
    2 Publications Verification

    Terrestrin A

    Deubiquitinase TNF Receptor E1/E2/E3 Enzyme Keap1-Nrf2 Inflammation/Immunology Cancer
    Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke [1] .
    Vialinin A
  • HY-134205A
    CBR-470-1
    3 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 [1] .
    CBR-470-1
  • HY-W017187

    Bacterial Drug Metabolite Keap1-Nrf2 Heme Oxygenase (HO) Infection
    2-tert-Butyl-1,4-benzoquinone is a food additive oxidant, an electrophilic metabolite of Butylated hydroxyanisole (HY-B1066), and an antibacterial agent. 2-tert-Butyl-1,4-benzoquinone reduces virulence factors, activates Nrf2, and induces S-arylation of its negative regulator Keap1. 2-tert-Butyl-1,4-benzoquinone induces HO-1. 2-tert-Butyl-1,4-benzoquinone exhibits quorum sensing inhibitory activity against Chromobacterium violaceum [1] .
    2-tert-Butyl-1,4-benzoquinone
  • 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 [1].
    TAT-14
  • 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-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-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
  • 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 [1].
    Nrf2 (69-84)
  • HY-141439

    Quinone Reductase Keap1-Nrf2 Inflammation/Immunology Cancer
    TBE 31 is a potent and orally active NQO1 inducer with an Dm value of 1.1 nM. TBE 31 also is a potent Nrf2 activator. TBE 31 reacts with cysteines of Keap1, impairing its ability to target nuclear factor-erythroid 2 p45-related factor 2 (Nrf2) for degradation. TBE 31 shows cytoprotective effects [1] .
    TBE 31
  • 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-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-P5909F

    Keap1-Nrf2 Others
    FITC-labeled Keap1-Nrf2 probe is aFITC-labeled Keap1-Nrf2 probe (HY-P5909).
    FITC-labeled Keap1-Nrf2 probe
  • HY-179398

    Keap1-Nrf2 Cancer
    Keap1-Nrf2-IN-29 (Compound 1a), a Curcumin (HY-N0005) analog, is a Keap1 protein inhibitor. Keap1-Nrf2-IN-29 exhibits significant inhibitory activity against A549, PC-3 and MCF-7 cells. Keap1-Nrf2-IN-29 can be used for the study of prostate cancer [1].
    Keap1-Nrf2-IN-29
  • HY-178054

    Keap1-Nrf2 Drug Derivative Neurological Disease
    LMDP10 is an orally active 3-amino quinazoline derivative with Keap1-Nrf2 pathway activation activity. LMDP10 binds to Keap1 to inhibit Keap1-Nrf2 interaction, thereby activating the Nrf2 pathway. LMDP10 elevates Nrf2, SOD, and GSH levels, reduces MDA and TNF-α levels, attenuates neurodegeneration, and improves memory function in Alzheimer’s disease (AD) rats. LMDP10 can be used for the study of AD [1].
    LMDP10
  • 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-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-178873

    PROTACs Ras Keap1-Nrf2 Cancer
    PROTAC K-Ras Degrader-7 is a potent PROTAC K-Ras degrader. PROTAC K-Ras Degrader-7 degrades K-Ras through recruiting the Keap1 E3 ubiquitin ligase. PROTAC K-Ras Degrader-7 can be used for research in pancreatic and colorectal cancers [1].
    PROTAC K-Ras Degrader-7
  • HY-139620

    PROTACs Cancer
    MS83 is a proof-of-concept PROTAC by linking the KEAP1 ligand to a BRD4/3/2 binder.
    MS83
  • 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-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-N10313

    Bcl-2 Family Keap1-Nrf2 Apoptosis Cancer
    Dehydrobruceine B, a quassinoid, can be isolated from Brucea javanica. Dehydrobruceine B shows a synergistic effect with Cisplatin (HY-17394) to induce apoptosis via mitochondrial method. Dehydrobruceine B increases apoptosis-inducing factor (AIF) and Bax expression and suppresses Keap1-Nrf2 [1].
    Dehydrobruceine B
  • HY-122054A

    Keap1-Nrf2 Cancer
    BPK-29 hydrochloride is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 hydrochloride impairs the anchorage-independent growth of KEAP1-mutant cancer cells [1].
    BPK-29 hydrochloride
  • HY-175548

    Keap1-Nrf2 Apoptosis Caspase Neurological Disease
    Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury [1].
    Nrf2 activator-21
  • HY-139047

    GLUT Cancer
    SW157765 is a selective non-canonical glucose transporter GLUT8 (SLC2A8) inhibitor. KRAS/KEAP1 double mutant NSCLC cells are selectively sensitive to the SW157765, due to the convergent consequences of dual KRAS and NRF2 modulation of metabolic and xenobiotic gene regulatory programs [1] .
    SW157765
  • HY-160876

    Keap1-Nrf2 E1/E2/E3 Enzyme Inflammation/Immunology
    BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury [1].
    BC-1901S
  • 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-169766

    Molecular Glues Keap1-Nrf2 Cancer
    VVD 065 is an orally active KEAP1-dependent NRF2 molecular glue degrader with a KEAP1 KD of 65 nM. VVD 065 covalently engages KEAP1 at Cys151, allosterically stabilizes KEAP1-CUL3 complex formation and enhances NRF2 polyubiquitination and proteasomal degradation. VVD 065 can be used for the research of esophageal squamous cell carcinoma, lung cancer, head-and-neck cancer, uterine cancers [1] .
    VVD 065
  • 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

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