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. Product Name Effect Purity Chemical Structure
  • HY-N1902S
    4-Hydroxyphenylacetic acid-d6
    		Activator 98.66%
    4-Hydroxyphenylacetic acid-d6 is the deuterium labeled 4-Hydroxyphenylacetic acid. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[1].
    4-Hydroxyphenylacetic acid-d<sub>6</sub>
  • HY-N6641
    Monascin
    		Activator 99.79%
    Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist.
    Monascin
  • HY-N4170
    Chebulic acid
    		Agonist 99.26%
    Chebulic acid is a phenolic acid compound isolated from Terminalia chebula with strong antioxidant activity, which breaks protein cross-links induced by advanced glycation end products (AGEs) and inhibits the formation of AGEs. Chebulic acid is effective in controlling elevated metabolic parameters, oxidative stress, and liver damage, supporting its beneficial role in asthma, diabetes, and liver protection.
    Chebulic acid
  • HY-119678
    Fortunellin
    		Activator
    Fortunellin, is a flavonoid, that can be isolated from the fruits of Fortunella margarita (kumquat). Fortunellin exhibits little toxicity to mice and suppresses inflammation and ROS generation in H9C2 cells induced by LPS. Fortunellin protects against fructose-induced inflammation and oxidative stress by enhancing AMPK/Nrf2 pathway. Fortunellin can be used for diabetic cardiomyopathy research.
    Fortunellin
  • HY-133114
    Ezetimibe ketone
    		Activator 99.97%
    Ezetimibe ketone (EZM-K) is a phase-I metabolite of Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator. Ezetimibe is a potent cholesterol absorption inhibitor.
    Ezetimibe ketone
  • HY-101140A
    KI696 isomer
    		Inhibitor 99.32%
    KI696 isomer is the less active isomer of KI696 (HY-101140). KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction.
    KI696 isomer
  • HY-N2995
    Poricoic acid A
    		Modulator 98.08%
    Poricoic acid A, isolated from Poria cocos, possesses anti-tumor activity. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis.
    Poricoic acid A
  • HY-N1970
    5,7-Dihydroxychromone
    		Activator 99.94%
    5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
    5,7-Dihydroxychromone
  • HY-N7617
    Toralactone
    		Inhibitor 98.75%
    Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
    Toralactone
  • HY-16561S
    Resveratrol-d4
    		Activator 99.36%
    Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
    Resveratrol-d<sub>4</sub>
  • HY-149010
    NXPZ-2
    		Inhibitor
    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.
    NXPZ-2
  • HY-134001
    CBR-470-2
    		Activator 99.45%
    CBR-470-2, a glycine-substituted analog, can activate NRF2 signaling. CBR-470-2 can be used for the research of modulation glycolysis.
    CBR-470-2
  • HY-P1328
    TAT-14
    		Activator 99.66%
    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.
    TAT-14
  • HY-101371
    Hesperin
    		Activator 99.20%
    Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
    Hesperin
  • HY-N0606
    Ginsenoside Rh3
    		Activator 99.95%
    Ginsenoside Rh3 is a bacterial metabolite of Ginsenoside Rg5. Ginsenoside Rh3 treatment in human retinal cells induces Nrf2 activation.
    Ginsenoside Rh3
  • HY-137315
    TML-6
    		Activator 99.01%
    TML-6, an orally active curcumin derivative, inhibits the synthesis of the β-amyloid precursor protein and β-amyloid (Aβ). TML-6 can upregulate Apo E, suppress NF-κB and mTOR, and increase the activity of the anti-oxidative Nrf2 gene. TML-6 has the potential for Alzheimer’s disease (AD) research.
    TML-6
  • HY-N1913A
    Danshensu sodium
    		Activator 98.00%
    Danshensu (Dan shen suan A) sodium, an orally active phenolic compound, can induce Nrf2/HO-1 activation and inhibition of NF-κB pathway. Danshensu sodium reduces reactive oxygen species (ROS) production, upregulates antioxidant defense mechanism and inhibits intrinsic apoptotic pathway. Danshensu sodium displays a potent antiviral activity against SARS-CoV-2 with EC50 of 0.97 μM. Danshensu sodium has anti-oxidation, anti-apoptosis, anti-lung inflammatory and has the potential for COVID-19, cardiovascular and cerebrovascular diseases research.
    Danshensu sodium
  • HY-N4028
    Hydrangenol
    		Inhibitor 99.63%
    Hydrangenol is an orally active antiphotoaging compound. It can be isolated from Hydrangea serrata leaves. Hydrangenol prevents wrinkle formation by reducing MMP and inflammatory cytokine expression and increasing moisturizing factors and antioxidant genes level.
    Hydrangenol
  • HY-122936
    Tanshindiol C
    		Activator 98.47%
    Tanshindiol C is a S-adenosylmethionine-competitive EZH2 (Histone Methyltransferase) inhibitor with an IC50 of 0.55 μM for inhibiting the methyltransferase activity. Tanshindiol C is also an activator of both Nrf2 and Sirtuin 1 (Sirt1) in macrophages. Tanshindiol C possesses anti-cancer activity, and can be used for atherosclerosis research.
    Tanshindiol C
  • HY-150579
    Keap1-Nrf2-IN-13
    		Inhibitor
    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.
    Keap1-Nrf2-IN-13
Cat. No. Product Name / Synonyms Application Reactivity