2. Signaling Pathways
  3. NF-κB
  4. Keap1-Nrf2

Keap1-Nrf2

Keap1-Nrf2

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Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS). Keap1 is an E3 ligase, which induces the degradation of Nrf2 by ubiquitin-proteasome system (UPS). Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. For this case, Nrf2 is an attractive molecule as a therapeutic target in cancer and a lot number of Nrf2 inhibitors are developed. What’s interesting, Nrf2 induction is also reported to be treatment strategies for accelerating the detoxification of carcinogens and protect the body from chemical carcinogenesis.

Cat. No. 상품명 효과 Purity Chemical Structure
  • HY-181818
    4,5-Dehydro-6-oxoallosecurinine
    		Activator
    4,5-Dehydro-6-oxoallosecurinine is a Keap1-Nrf2 pathway activator. 4,5-Dehydro-6-oxoallosecurinine promotes the nuclear translocation of Keap1-Nrf2, and induces the expression of antioxidant and cytoprotective genes. 4,5-Dehydro-6-oxoallosecurinine reduces the production of NO, and decreases the levels of iNOS, TNF-α, IL-6 and IL-1β in LPS-stimulated microglia. 4,5-Dehydro-6-oxoallosecurinine can be used for the research of neurodegenerative diseases.
    4,5-Dehydro-6-oxoallosecurinine
  • HY-P11124
    MGF24
    		Activator
    MGF24 is a modified protease-resistant MGF derivative. MGF24 protects dopaminergic neurons from 6-Hydroxydopamine (6-OHDA) (HY-113028)-induced apoptosis by inducing Heme oxygenase-1 (HO-1). MGF24 activates PKC-ε, which in turn activates Nrf2, up-regulating HO-1. MGF24 has neuroprotective activity and reduces myocardial infarct size in sheep models of myocardial ischemia. MGF24 can be used for neurological diseases like stroke, nerve injury and amyotrophic lateral sclerosis research.
    MGF24
  • HY-169315
    Nrf2 activator 17
    		Activator
    Nrf2 activator 17 (compound 10) is an Nrf2 activator that inhibits the interaction between Keap1 and Nrf2 with an IC50 of < 0.1 pM. Additionally, Nrf2 activator 17 has an EC50 of < 10 μM in HepG2 cells.
    Nrf2 activator 17
  • HY-161783
    HDAC6-IN-45
    		Activator
    HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability.
    HDAC6-IN-45
  • HY-N6953R
    Garcinone D (Standard)
    		Activator
    Garcinone D (Standard) is the analytical standard of Garcinone D (HY-N6953). This product is intended for research and analytical applications. Garcinone D is an activator of the STAT3/Cyclin D1 and Nrf2/HO-1 pathways, and an inhibitor of CDK2/CyclinE1 (IC50 for CDK2/CyclinE1 is 28.23 μM). Garcinone D promotes neural stem cell proliferation by activating STAT3 phosphorylation and Cyclin D1 expression and enhancing the Nrf2/HO-1 signaling pathway. In addition, Garcinone D blocks the tumor cell cycle by inhibiting CDK2/CyclinE1. Garcinone D can promote the proliferation of C17.2 neural stem cells and inhibit prostate and breast cancer.
    Garcinone D (Standard)
  • HY-181765
    TLR4/NF-κB-IN-2
    		Activator
    TLR4/NF-κB-IN-2 is an orally active TLR4/NF-κB inhibitor and Nrf2/HO-1 activator. TLR4/NF-κB-IN-2 combats oxidative stress and exerts anti-inflammatory effects by regulating the Nrf2/HO-1 and TLR4/NF-κB pathways. TLR4/NF-κB-IN-2 reduces Aβ aggregation and protects neurons. TLR4/NF-κB-IN-2 can be used in the research of Alzheimer's disease.
    TLR4/NF-κB-IN-2
  • HY-161643
    S21-1011
    		Activator
    S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model.
    S21-1011
  • HY-175675
    P2Y1 antagonist 4
    		Activator
    P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction.
    P2Y1 antagonist 4
  • HY-N10431
    Stigmane B
    		Activator
    Stigmane B (Compound 2) is a nuclear factor E2-related factor (Nrf2) activator. Stigmane B downregulates apoptosis and reactive oxygen species (ROS) generation, and increases antioxidant enzyme activities. Stigmane B shows neuroprotective effects.
    Stigmane B
  • HY-N0512R
    Loganin (Standard)
    		Activator
    Loganin (Standard) is the analytical standard of Loganin. This product is intended for research and analytical applications. Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI).
    Loganin (Standard)
  • HY-176146
    Keap1/Nrf2/ARE activator 1
    		Activator
    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-N17603
    Ginnalin A
    		Activator
    Ginnalin A (Acertannin) is a Nrf2 activator. Ginnalin A shows antiproliferative activity against HCT116, SW480 and SW620 cells with IC50 values of 24.8, 22.0, and 39.7 μM, respectively. Ginnalin A can induce cancer cells S phase arrest. Ginnalin A can activate the p62-Keap1-Nrf2 signaling pathway, significantly upregulate the mRNA and protein expression of Nrf2, HO-1, and NQO1, and promote the transport of Nrf2 from the cytoplasm to the nucleus. Ginnalin A can be used for the research of colon cancer.
    Ginnalin A
  • HY-175217
    Nrf2 activator-20
    		Activator
    Nrf2 activator-20 is a potent Nrf2 activator with anti-inflammatory and antioxidant activities. Nrf2 activator-20 activates the anti-inflammatory pathway by interfering with the Keap1-Nrf2 interaction and is beneficial in vivo. Nrf2 activator-20 can be used for the study of acute respiratory distress syndrome (ARDS) and ischemia-reperfusion injury.
    Nrf2 activator-20
  • HY-W001083S1
    3-Hydroxyphenylacetic acid-d5
    		Activator
    2-(3-Hydroxyphenyl-2,4,6-d3)acetic-2,2-d2 acid is the deuterium labeled 3-Hydroxyphenylacetic acid (HY-W001083). 3-Hydroxyphenylacetic acid is an orally active flavonoid metabolite produced by intestinal flora, with blood pressure-lowering activity. 3-Hydroxyphenylacetic acid can also inhibit ferroptosis by upregulating the expression of GPX4, thereby improving spermatogenic dysfunction in aged mice. In addition, abnormal levels of 3-Hydroxyphenylacetic acid are closely related to certain diseases, such as autism spectrum disorders.
    3-Hydroxyphenylacetic acid-d<sub>5</sub>
  • HY-N0638R
    Dendrobine (Standard)
    		Activator
    Dendrobine (Standard) is the analytical standard of Dendrobine. This product is intended for research and analytical applications. Dendrobine is an alkaloid isolated from Dendrobium nobile. Dendrobine possesses antiviral activity against influenza A viruses, with IC50s of 3.39 μM, 2.16 μM and 5.32 μM for A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2), respectively. Dendrobine activates the JNK/p38/Nrf2 signaling pathway. Dendrobine exhibits antiviral, antitumor, anti-inflammatory, and neuroprotective properties.
    Dendrobine (Standard)
  • HY-W104821
    Rosolic acid
    		Activator
    Rosolic Acid is an activator of Nrf2, as well as its downstream targets. Rosolic Acid increases the levels of angiogenic factors, decreases inflammation (TNF-α and IL-1β) and apoptotic markers (CXCL10 and CCL2). Rosolic Acid restores the function of pancreatic cells and protects endothelial cells (ECs) from endoplasmic reticulum stressed.
    Rosolic acid
  • HY-124345
    2-Trifluoromethyl-2'-methoxychalcone
    		Activator
    2-Trifluoromethyl-2'-methoxychalcone is a chalcone derivative. 2-Trifluoromethyl-2'-methoxychalcone is a potent Nrf2 activator. 2-Trifluoromethyl-2'-methoxychalcone can be used for oxidative stress and inflammation related diseases research.
    2-Trifluoromethyl-2'-methoxychalcone
  • HY-P1328A
    TAT-14 TFA
    		Activator
    TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
    TAT-14 TFA
  • HY-W001083R
    3-Hydroxyphenylacetic acid (Standard)
    		Activator
    3-Hydroxyphenylacetic acid (Standard) is the analytical standard of 3-Hydroxyphenylacetic acid (HY-W001083). This product is intended for research and analytical applications. 3-Hydroxyphenylacetic acid is an orally active flavonoid metabolite produced by intestinal flora, with blood pressure-lowering activity. 3-Hydroxyphenylacetic acid can also inhibit ferroptosis by upregulating the expression of GPX4, thereby improving spermatogenic dysfunction in aged mice. In addition, abnormal levels of 3-Hydroxyphenylacetic acid are closely related to certain diseases, such as autism spectrum disorders.
    3-Hydroxyphenylacetic acid (Standard)
  • HY-112675R
    4-Octyl itaconate (Standard)
    		Activator
    4-Octyl itaconate (Standard) is the analytical standard of 4-Octyl itaconate. This product is intended for research and analytical applications. 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 (Standard)
Cat. No. 상품명 / Synonyms Application Reactivity