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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
31 Results for "
Nrf2 degrader
" in MedChemExpress (MCE) Product Catalog:
Products (31)
31 Results for "Nrf2 degrader" in MCE Product Catalog:
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23 Publications Verification
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KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .
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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 .
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1 Cited Publications
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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 .
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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 .
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1 Cited Publications
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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) .
Cat. No.: HY-162307
CAS No.: 3025286-00-1
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Nrf2 degrader 1 (compound 1) is a PROTAC Nrf2 degrader with a DC50 of 0.1-1 μM in huH1 cells. 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 can be used for the study of liver cancer, non-small cell lung cancer (NSCLC) and squamous cell carcinoma of lung cancer .
Cat. No.: HY-159641
CAS No.: 3034880-93-5
Synonyms: BAY-3605349
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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 .
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Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
WS3 is an allosteric inhibitor of 14-3-3 (14-3-3ζ: Kd = 2.29 μM). WS3 activates GSK3β by disrupting the binding of 14-3-3-pGSK3β, promotes the ubiquitination and degradation of NRF2, and inhibits the NRF2-ARE signaling pathway (IC50 = 135 nM). It exerts antioxidant inhibition and chemotherapeutic/ferroptosis sensitizing effects in tumors with hyperactivated NRF2. WS3 binds to EBP1/IKKε and promotes the proliferation of β cells and retinal pigment epithelial (RPE) cells, which can be applied to islet regeneration and RPE expansion transplantation . WS3 is applicable to research related to age-related macular degeneration, retinal degeneration and non-small cell lung cancer .
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KI696 isomer is an isomer of KI696 (HY-101140). KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .
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MSU38225 is a selective Nrf2 inhibitor. MSU38225 increases ROS levels by inhibiting antioxidant production. MSU38225 arrests cells at the G2/M phase, enhances cellular sensitivity to chemotherapeutic agents, and exerts synergistic effects with Carboplatin (HY-17393) and 5-fluorouracil (HY-90006). MSU38225 exhibits anticancer activity against lung cancer. MSU38225 can be used in research related to non-small cell lung cancer .
Synonyms: ASC-JM17; ALZ-003
Target:
Keap1-Nrf2 Androgen Receptor HSP Mitophagy Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Autophagy
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Rosolutamide (ASC-JM17) is an orally active Nrf1/Nrf2 activator. Rosolutamide activates Hsf1 pathways, upregulates proteasome subunits and antioxidant enzymes, induces proteasome complex structural rearrangement, and enhances ubiquitin-proteasome system-mediated degradation. Rosolutamide reduces mutant androgen receptor and ataxin-3 aggregates, restores mitochondrial function, attenuates reactive oxygen species (ROS) levels, induces apoptosis and ferroptosis, and inhibits cancer cell growth. Rosolutamide can be used for the research of spinal and bulbar muscular atrophy, Huntington’s disease, and temozolomide-resistant glioblastoma .
Cat. No.: HY-175209
CAS No.: 2417486-06-5
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Nrf2-IN-4 is a Nrf2 inhibitor. Nrf2-IN-4 induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 demonstrates significant antitumor efficacy. Nrf2-IN-4 can be used for the study of breast cancer .
Cat. No.: HY-17655
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TBE56, a molecular glue, is a BACH1 degrader, with an EC50 of 44 nM. TBE56 is a weak NRF2 inducer and the biotinylated TBE31. TBE56 interacts and promotes the
degradation of BACH1 via a mechanism involving the E3 ligase FBX022. TBE56 reduces intracellular Fe 2+ accumulation, ROS generation, and malondialdehyde (MDA) content, while increasing GSH/GSSG ratio and upregulating GPX4 in Prominin-2-overexpressed BMSCs. TBE56 significantly ameliorates intervertebral disc degeneration (IVDD) in puncture-induced SD rat IVDD model. TBE56 can be used for the study of intervertebral disc degeneration (IVDD) .
Cat. No.: HY-N5008
CAS No.: 146100-02-9
Cat. No.: HY-141439
CAS No.: 936475-62-6
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TBE 31 is an orally active Keap1/Nrf2 pathway activator and NQO1 inducer with a Dm value of 1.1 nM for NQO1. TBE 31 binds to cysteine residues of Keap1, inhibits ubiquitination and degradation of Nrf2, thereby activating the expression of ARE-dependent genes. TBE 31 induces cytoprotective enzymes including NQO1 and GST isoforms, promotes Nrf2 accumulation, and upregulates Nrf2-regulated genes related to antioxidation and lipid metabolism. TBE 31 inhibits pro-inflammatory responses, formation of AFB1-DNA adducts, endoplasmic reticulum stress, cell apoptosis (apoptosis), hepatic fibrosis, oxidative stress, and the expression of ChREBP. TBE 31 reduces the number of tumors in a mouse model of ultraviolet-induced skin carcinogenesis. TBE 31 enhances nerve growth factor-induced neurite outgrowth. TBE 31 attenuates LPS-induced serum TNF-α levels and immobility time in mice. TBE 31 can be used in research related to liver cancer, skin cancer, inflammation-related depression, and non-alcoholic steatohepatitis .
Cat. No.: HY-175209A
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Nrf2-IN-4 (Compound PhcY) hydrobromide is a Nrf2 inhibitor. Nrf2-IN-4 hydrobromide induces ferroptosis via NRF2 inhibition. Nrf2-IN-4 hydrobromide disrupts cellular iron homeostasis, facilitates ferritin degradation, and ultimately triggers ferroptosis. Nrf2-IN-4 hydrobromide induces lysosome activation by promoting iron-dependent ROS production and lysosomal acidification. Nrf2-IN-4 hydrobromide demonstrates significant antitumor efficacy. Nrf2-IN-4 hydrobromide can be used for the study of breast cancer .
Cat. No.: HY-184846
CAS No.: 3025286-29-4
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PROTAC Nrf2 degrader-1 is a PROTAC degrader targeting Nrf2, with IC50 values of 10 nM and 3 nM in A549 cells and LK-2 cells, respectively. PROTAC Nrf2 degrader-1 can be used in cancer research .
Cat. No.: HY-178875
CAS No.: 3082764-64-2
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Nrf2 activator-22, a Nrf2 activator, is a PROTAC target protein ligand. Nrf2 activator-22 can be used for synthesis PROTAC K-Ras Degrader-7 (HY-178873) .
Cat. No.: HY-169766
CAS No.: 3034876-85-9
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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 .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
