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-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-160876
    BC-1901S
    		Activator 99.81%
    BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury.
    BC-1901S
  • HY-N8698
    Picein
    		Activator 99.98%
    Picein is an antioxidant and anti-inflammatory agent. Picein can be isolated from the leaves of Picrorhiza kurroa. Picein reduces MDA levels and increases the levels of SOD, GPX and TAC. Picein alleviates oxidative stress and promotes bone regeneration in osteoporotic bone defects by inhibiting Ferroptosis (via activation of the Nrf2/HO-1/GPX4 pathway). Picein prevents scopolamine (HY-N0296)-induced passive avoidance memory impairment in rats. Picein can be used in research related to osteoporotic bone defects and Alzheimer's disease.
    Picein
  • HY-W017187
    2-tert-Butyl-1,4-benzoquinone
    		Activator 99.00%
    2-tert-Butyl-1,4-benzoquinone is a food additive oxidant, an electrophilic metabolite of Butylated hydroxyanisole (HY-B1066), and an antibacterial agent. 2-tert-Butyl-1,4-benzoquinone reduces virulence factors, activates Nrf2, and induces S-arylation of its negative regulator Keap1. 2-tert-Butyl-1,4-benzoquinone induces HO-1. 2-tert-Butyl-1,4-benzoquinone exhibits quorum sensing inhibitory activity against Chromobacterium violaceum.
    2-tert-Butyl-1,4-benzoquinone
  • HY-N0761A
    trans-Isoferulic acid
    		Activator 99.93%
    trans-Isoferulic acid (trans-3-Hydroxy-4-methoxycinnamic acid) is an aromatic acid that exhibits anti-inflammatory activity. trans-Isoferulic acid dephosphorylates PI3K/Akt, suppresses LPS (HY-D1056)-induced NF-κB activation, enhances Nrf2 activity, downregulates iNOS and COX-2 expression, induces HO-1 expression, inhibits NO and PGE2 production, and scavenges hydroperoxyl radical. trans-Isoferulic acid can be used for research of inflammatiory diseases.
    trans-Isoferulic acid
  • HY-17363R
    Dimethyl fumarate (Standard)
    		Activator
    Dimethyl fumarate (Standard) is the analytical standard of Dimethyl fumarate. This product is intended for research and analytical applications. Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research.
    Dimethyl fumarate (Standard)
  • HY-N0440R
    Germacrone (Standard)
    		Activator
    Germacrone (Standard) is an analytical standard of Gemmacrone (HY-N0440). This product is intended for research and analytical applications. Germacrone (Standard) is a sesquiterpene compound with multiple biological activities. Germacrone (Standard) inhibits the H1N1 and H3N2 influenza A viruses and the influenza B virus. Germacrone (Standard) blocks the progressionof arthritis by regulating Th1/Th2 balance and inhibiting NF-κB signaling. Germacrone (Standard) can arrest the cell cycle at G0/G1 and G2/M phases and induce apoptosis in breast cancer cells. Germacrone (Standard) inhibits 5α-reductase and has anti-androgenic effect. Germacrone (Standard) has neuroprotective functions and can be used for the study of traumatic brain injury (TBI). Germacrone (Standard) also has antioxidant activity.
    Germacrone (Standard)
  • HY-100573A
    (E/Z)-Necrosulfonamide
    		Activator 98.03%
    (E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    (E/Z)-Necrosulfonamide
  • HY-121811
    Pongamol
    		Activator 99.81%
    Pongamol (Lanceolatin C) is an orally active flavonoid with an IC50 of 75 μM and a Ki of 58 μM against PTPase-1B, and an IC50 of 103.5 μM against intestinal α-Glycosidase. Pongamol reduces the release of IL‑1β, TNF‑α, COX‑2 and iNOS in cells, reverses the nuclear translocation of NF‑κB, and upregulates the levels of Beclin 1 and LC3 Ⅱ/LC3 Ⅰ. Pongamol promotes glucose uptake by increasing the level of GLUT4 on the surface of skeletal muscle cells. Pongamol inhibits epithelial-mesenchymal transition by suppressing the FAK/Akt-mTOR signaling pathway. Pongamol inhibits neuronal cytotoxicity, suppresses cell apoptosis and extends the lifespan of Caenorhabditis elegans by activating the MAPKs/Nrf2 signaling pathway. Pongamol exerts hypoglycemic effects in diabetic mouse models. Pongamol exhibits antibacterial activity. Pongamol alleviates oxidative stress, neuroinflammation, Aβ deposition and excessive phosphorylation of Tau Protein, and restores autophagy function in Alzheimer's disease mouse models by inhibiting the Akt/mTOR signaling pathway. Pongamol is applicable to research related to Alzheimer's disease, type 2 diabetes, non-small cell lung cancer and postprandial hyperglycemia.
    Pongamol
  • HY-145390A
    (R,R)-Nrf2 activator-1
    		Activator
    (R,R)-Nrf2 activator-1 is the enantiomer of Nrf2 activator-1. Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the research of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis.
    (R,R)-Nrf2 activator-1
  • HY-124481
    Oleocanthal
    		Activator ≥99.0%
    Oleocanthal is an orally active phenolic seciridoid compound. Oleocanthal can be extracted from olive oil. Oleocanthal inhibits COX-1 and COX-2, reduces ROS and NO, and upregulates Nrf-2 and HO-1. Oleocanthal reduces Aβ deposition. Oleocanthal exhibits anti-Leishmania activity against promastigotes and amastigotes of L. major, with IC50 values of 18.7 and 87 μg/mL, respectively. Oleocanthal exhibits anticancer activity against colon, breast, liver, and melanoma cancers. Oleocanthal also exhibits anti-inflammatory and neuroprotective properties. Oleocanthal can be used in Alzheimer's disease research.
    Oleocanthal
  • HY-14645A
    (+)-DHMEQ
    		Activator 99.18%
    (+)-DHMEQ is an activator of antioxidant transcription factor Nrf2. (+)-DHMEQ is the enantiomer of (-)-DHMEQ. (-)-DHMEQ inhibits NF-kB than its enantiomer (+)-DHMEQ.
    (+)-DHMEQ
  • HY-145390
    Nrf2 activator-1
    		Activator 98.66%
    Nrf2 activator-1 is a potent activator of NF-E2 related factor 2 (Nrf2). Nrf2 activator-1 has the potential for the research of COPD and other respiratory diseases, including asthma, Acute Lung Injury (ALI), Acute Respiratory Distress Syndrome (ARDS) and pulmonary fibrosis (extracted from patent WO2018109647A1).
    Nrf2 activator-1
  • HY-121523
    MIND4-17
    		Activator 99.05%
    MIND4-17 is a potent NRF2 activator that covalently modifies a C151 residue of Keap1. MIND4-17 disrupts Keap1-Nrf2 association, leading to Nrf2 protein stabilization and nuclear translocation. MIND4‐17 exerts potent antioxidant activity.
    MIND4-17
  • HY-137315
    TML-6
    		Activator 98.34%
    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-100573S
    Necrosulfonamide-d4
    		Activator 99.65%
    Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide (HY-100573). Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    Necrosulfonamide-d<sub>4</sub>
  • HY-164826
    Acetyl zingerone
    		Activator 99.34%
    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-148480
    Nrf2 activator-6
    		Activator
    Nrf2 activator-6, a tetrahydroisoquinoline compound, is a Nrf2 activator. Nrf2 activator-6 has an IC50 of 5 nM for inhibiting the Kelch domain-Nrf2 interaction (WO2021214470A1; Example 4).
    Nrf2 activator-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-17376R
    Ezetimibe (Standard)
    		Activator
    Ezetimibe (Standard) is the analytical standard of Ezetimibe. This product is intended for research and analytical applications. 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 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity