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

Keap1-Nrf2

Keap1-Nrf2 is the major regulator of cytoprotective responses to oxidative and electrophilic stress. Kelch-like ECH-associated protein 1 is a protein that in humans is encoded by the Keap1 gene. Keap1 has been shown to interact with Nrf2, a master regulator of the antioxidant response, which is important for the amelioration of oxidative stress. Under quiescent conditions, Nrf2 is anchored in the cytoplasm through binding to Keap1, which, in turn, facilitates the ubiquitination and subsequent proteolysis of Nrf2. Such sequestration and further degradation of Nrf2 in the cytoplasm are mechanisms for the repressive effects of Keap1 on Nrf2. because Nrf2 activation leads to a coordinated antioxidant and anti-inflammatory response, and Keap1 represses Nrf2 activation, Keap1 has become a very attractive drug target.

Keap1-Nrf2 Related Products (27):

Cat. No. Product Name Effect Purity
  • HY-100523
    ML385 Inhibitor 99.59%
    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
  • HY-N0005
    Curcumin Activator 99.66%
    Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
  • HY-100489
    TBHQ Activator >98.0%
    TBHQ is an antioxidant that activates Nrf2.
  • HY-13324
    Bardoxolone methyl Activator 99.72%
    Bardoxolone is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
  • HY-112675
    4-Octyl Itaconate Activator 99.64%
    4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1.
  • HY-N0682
    Pyridoxine hydrochloride 99.75%
    Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
  • HY-Z0548
    Methyl 3,4-dihydroxybenzoate Agonist
    Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester;Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect.
  • HY-N1902
    4-Hydroxyphenylacetic acid Activator >98.0%
    4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2.
  • HY-12212
    RTA-408 Activator 98.96%
    RTA-408 is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO).
  • HY-101140
    KI696 Inhibitor 99.72%
    KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
  • HY-17363
    Dimethyl fumarate Activator >98.0%
    Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
  • HY-15725
    CDDO-Im Activator 98.20%
    CDDO-Im (CDDO-imidazolide) is an activator of Nrf2 and PPAR, with Kis of 232 and 344 nM for PPARα and PPARγ.
  • HY-14909
    Bardoxolone Activator 99.14%
    Bardoxolone is a novel nuclear regulator factor (Nrf-2) activator.
  • HY-17376
    Ezetimibe Activator 99.76%
    Ezetimibe (SCH 58235) is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor.
  • HY-19734
    NK-252 Activator 99.96%
    NK-252 is a potential Nrf2 activator, which exhibits a great Nrf2-activating potential.
  • HY-19543
    Brusatol Inhibitor 99.89%
    Brusatol (NSC 172924), isolated from the Brucea javanica plant, inhibits Nrf2.
  • HY-N1913
    Danshensu Activator >98.0%
    Danshensu, an active ingredient of Salvia miltiorrhiza, shows wide cardiovascular benefit by activating Nrf2 signaling pathway.
  • HY-B2230
    Hinokitiol Inhibitor >98.0%
    Hinokitiol is a component of essential oils isolated from Chymacyparis obtusa, reduces Nrf2 expression, and decreases DNMT1 and UHRF1 mRNA and protein expression, with anti-infective, anti-oxidative, and anti-tumor activities.
  • HY-12213
    CDDO-EA Activator 99.32%
    CDDO-EA is an NF-E2 related factor 2/antioxidant response element (Nrf2/ARE) activator.
  • HY-N0290
    Mangiferin Activator 99.84%
    Mangiferin is a Nrf2 activator. Mangiferin suppresses nuclear translocation of the NF-κB subunits p65 and p50.
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