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Nrf2 target genes

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12

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Cat. No. Product Name Target Research Areas Chemical Structure
  • 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) .
    Citraconic acid
  • HY-112671
    CDDO-dhTFEA

    RTA dh404

    		 Keap1-Nrf2 NF-κB Apoptosis Cardiovascular Disease Inflammation/Immunology
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
    CDDO-dhTFEA
  • HY-147517
    Keap1-Nrf2-IN-9

    		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-171705
    KMS99220

    		Keap1-Nrf2 AMPK JNK IKK p38 MAPK NO Synthase α-synuclein Interleukin Related Neurological Disease
    KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease .
    KMS99220
  • 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-164826
    Acetyl zingerone

    		Interleukin Related Reactive Oxygen Species (ROS) MMP Pyroptosis Ferroptosis Notch Keap1-Nrf2 PINK1/Parkin Mitophagy Caspase Apoptosis Inflammation/Immunology Cancer
    Acetyl zingerone is an analog of Zingerone (HY-14621). Acetyl zingerone downregulates the expression of ROS metabolism-related genes, fibroblast senescence-related genes, keratinocyte differentiation-related genes, and IL-17A target genes. Acetyl zingerone inhibits the activities of MMP-1, MMP-3, and MMP-12, as well as the activation of NLRP3 inflammasome, pyroptosis (pyroptosis), ferroptosis (ferroptosis), cartilage destruction, and UVA-induced cyclobutane pyrimidine dimer formation. Acetyl zingerone upregulates the expression of collagen, proteoglycan, extracellular matrix glycoprotein, Notch pathway, and GPX4 gene, activates Nrf2 and HO-1, induces extracellular matrix synthesis and PINK1/Parkin-mediated mitophagy (mitophagy), and promotes chondrocyte survival. Acetyl zingerone alleviates the progression of osteoarthritis in mice . Acetyl zingerone can be used in research related to skin aging, inflammatory skin diseases, osteoarthritis, melanoma, and non-melanoma skin cancer .
    Acetyl zingerone
  • HY-N1902R
    4-Hydroxyphenylacetic acid (Standard)

    		Reference Standards Keap1-Nrf2 Endogenous Metabolite Metabolic Disease
    4-Hydroxyphenylacetic acid (Standard) is the analytical standard of 4-Hydroxyphenylacetic acid. This product is intended for research and analytical applications. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2 . IC50 & Target:Nrf2 In Vivo: 4-Hydroxyphenylacetic acid (6, 12, or 25 mg/kg) increases Nrf2 translocation to the nucleus and enhances the activity of phase II and antioxidant enzymes. The protein levels of nuclear Nrf2 are increased by 170% and 230% in pre-treated 12 and 25 mg/kg 4-Hydroxyphenylacetic acid groups, respectively, compared with the control group.The 4-Hydroxyphenylacetic acid pretreatment at a final dose of 25 mg/kg markedly and selectively up-regulated the target genes of phase II enzymes and resulted in higher up-regulation than that of the control group by 270%, 400%, and 500% or UGT1A1, UGT1A9, and SULT2A1, respectively. 4-Hydroxyphenylacetic acid also suppresses the expression of CYP2E1 .
    4-Hydroxyphenylacetic acid (Standard)
  • HY-156240
    DI-1548

    		E1/E2/E3 Enzyme Keap1-Nrf2 Metabolic Disease
    DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research .
    DI-1548
  • HY-113298R
    Citraconic acid (Standard)

    Methylmaleic acid (Standard)

    		 Reference Standards NOD-like Receptor (NLR) Keap1-Nrf2 Reactive Oxygen Species (ROS) Cardiovascular Disease Inflammation/Immunology
    Citraconic acid (Methylmaleic acid) (Standard) is the analytical standard of Citraconic acid (HY-113298). This product is intended for research and analytical applications. Citraconic 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) .
    Citraconic acid (Standard)
  • HY-182818
    SH494

    		p38 MAPK Keap1-Nrf2 Reactive Oxygen Species (ROS) Metabolic Disease
    SH494 is a p38 MAPK inhibitor and Nrf2 pathway activator. SH494 inhibits RANKL-induced phosphorylation of p38 and disrupts the MAPK cascade associated with osteoclastogenesis. SH494 activates the Nrf2 pathway, upregulates downstream target genes and induces the expression of cytoprotective enzymes. SH494 reduces intracellular ROS accumulation and restores mitochondrial membrane potential (ΔΨm) to normal. SH494 decreases osteoclast activity and alleviates osteoporosis symptoms in ovariectomized mice. SH494 can be used for research on osteoporosis .
    SH494
  • HY-183326
    Isosorbide di-(methyl fumarate)

    IDMF

    		 Keap1-Nrf2 Inflammation/Immunology
    Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris .
    Isosorbide di-(methyl fumarate)
  • HY-13689G
    Go 6983

    		PKC Histone Methyltransferase DNA Methyltransferase DNA/RNA Synthesis Inflammation/Immunology
    Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury .
    Go 6983

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