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-120912
    Gingerenone A
    		Activator 99.49%
    Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale.
    Gingerenone A
  • HY-100375
    Diroximel fumarate
    		Activator 99.90%
    Diroximel fumarate (ALKS 8700) is an orally-active and well-tolerated monomethyl fumarate (MMF) proagent in a controlled-release formulation. Diroximel fumarate is considered as active equivalent to its active metabolite dimethyl fumarate (DMF). Diroximel fumarate has a favorable safety and efficacy profile, has the potential for the study of multiple sclerosis (MS). Diroximel fumarate is a Nrf2 activator that alleviate MGO-induced pain hypersensitivity.
    Diroximel fumarate
  • HY-N4113
    Glycycoumarin
    		Modulator 99.89%
    Glycycoumarin is a potent antispasmodic agent. Glycycoumarin is a major bioactive coumarin of licorice and exhibits antispasmodic activity. Glycycoumarin also has hepatoprotective effect. Glycycoumarin can be used for the research of abdominal pain and liver diseases.
    Glycycoumarin
  • HY-153340
    I-152
    		Activator 98.78%
    I-152 is a conjugate containing N-acetyl-cysteine (NAC) and cysteamine (MEA). I-152 activates NRF2 and ATF4 signals. I-152 has anti-proliferative properties.
    I-152
  • HY-131592
    Tricetin
    		Inhibitor 99.19%
    Tricetin is a potent competitive inhibitor of the Keap1-Nrf2 Protein Protein Interaction (PPI). Tricetin protects against 6-OHDA-induced neurotoxicity in Parkinson's disease model by activating Nrf2/HO-1 signaling pathway and preventing mitochondria-dependent apoptosis pathway.
    Tricetin
  • 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-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-N7617
    Toralactone
    		Inhibitor 98.75%
    Toralactone, isolated from Cassia obtusifolia, mediates hepatoprotection via an Nrf2-dependent anti-oxidative mechanism.
    Toralactone
  • HY-N1970
    5,7-Dihydroxychromone
    		Activator 99.98%
    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-101371
    Hesperin
    		Activator
    Hesperin is a bioactive ingredient present in Japanese horseradish (wasabi) and has been shown to be an Nrf2 activator.
    Hesperin
  • 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-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-77293
    (E)-[6]-Dehydroparadol
    		Activator
    (E)-[6]-Dehydroparadol, an oxidative metabolite of [6]-Shogaol (HY-14616), is a potent Nrf2 activator. (E)-[6]-Dehydroparadol can inhibit the growth and induce the apoptosis of human cancer cells.
    (E)-[6]-Dehydroparadol
  • HY-N0162R
    Luteolin (Standard)
    		Inhibitor 98.72%
    Luteolin (Standard) is the analytical standard of Luteolin. This product is intended for research and analytical applications. Luteolin (Luteoline), a flavanoid compound, is a potent Nrf2 inhibitor. Luteolin has anti-inflammatory, anti-cancer properties, including the induction of apoptosis and cell cycle arrest, and the inhibition of metastasis and angiogenesis, in several cancer cell lines, including human non-small lung cancer cells.
    Luteolin (Standard)
  • HY-N2995
    Poricoic acid A
    		Modulator ≥98.0%
    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-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-N3847
    Eriodictyol-7-O-glucoside
    		Activator 99.82%
    Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is a potent free radical scavenger. Eriodictyol-7-O-glucoside is also an Nrf2 activator, confers protection against Cisplatin-induced toxicity.
    Eriodictyol-7-O-glucoside
  • HY-17376S1
    Ezetimibe-d4-1
    		Activator 99.25%
    Ezetimibe-d4-1 is deuterium labeled Ezetimibe. Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
    Ezetimibe-d<sub>4</sub>-1
  • HY-14645A
    (+)-DHMEQ
    		Activator 99.33%
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
    (+)-DHMEQ
Cat. No. Product Name / Synonyms Application Reactivity