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-B1000R
    Selenomethionine (Standard)
    		Activator
    Selenomethionine (Standard) is the analytical standard of Selenomethionine. This product is intended for research and analytical applications. Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity[1][2][3].
    Selenomethionine (Standard)
  • HY-142026
    Vitisin A
    		Activator
    Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC50 values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.
    Vitisin A
  • HY-N1244
    Sarmentosin
    		Activator
    Sarmentosin is an activator of Nrf2. Sarmentosin inhibits mTOR signaling and induces autophagy-dependent apoptosis in human HCC cells.
    Sarmentosin
  • HY-118828B
    12-Oxo phytodienoic acid (≥90%)
    		Activator
    12-Oxo phytodienoic acid (≥90%) (12-OPDA (≥90%)) is a plant lipid-derived anti-inflammatory compound. 12-Oxo phytodienoic acid (≥90%) induces the expression of SOCS-1 and inhibits LPS (HY-D1056)-induced activation of the NF-κB and p38 MAPK signaling pathways. 12-Oxo phytodienoic acid (≥90%) inhibits LPS-induced expression of IL-6 and TNF-α, and reduces LPS-induced NO production by decreasing iNOS levels. 12-Oxo phytodienoic acid (≥90%) induces activation of the Nrf2 signaling cascade. 12-Oxo phytodienoic acid (≥90%) can be used for the research of neurodegenerative diseases.
    12-Oxo phytodienoic acid (≥90%)
  • HY-N8284
    Tomentosin
    		Activator 98.95%
    Tomentosin is an orally active natural sesquiterpenoid lactone. Tomentosin exhibits multiple activities such as anti-tumor, anti-fungal, anti-inflammatory, anti-oxidant and neuroprotective effects. Tomentosin can inhibit tumor cell proliferation, migration and invasion, and induce apoptosis. Tomentosin can be used in the research of tumors, inflammation and nervous system diseases.
    Tomentosin
  • HY-124834
    Nrf2 activator-10
    		Activator 98.65%
    Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent inducer for antioxidant response element (ARE) (EC50 is 2.7 μM) and an activator for Nrf2. Nrf2 activator-10 modifies Keap1, blocks Cul3-Keap1 ubiquitin ligase complex, activates the transcription of Nrf2. Nrf2 activator-10 protects cells from H2O2-induced apoptosis.
    Nrf2 activator-10
  • HY-115849
    Nrf2-Activator-12G
    		Activator 99.57%
    Nrf2-Activator-12G (compd 12g) is an activator of Nrf2. Nrf2-Activator-12G induces the expression of nrf2-dependentantioxidant enzymes at both mRNA and protein levels in DAergic neuronal cell. Nrf2-Activator-12G can used in study Parkinson’s Disease.
    Nrf2-Activator-12G
  • HY-B0916
    Propoxur
    		Activator 99.43%
    Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.
    Propoxur
  • HY-178054
    LMDP10
    		Activator 99.91%
    LMDP10 is an orally active 3-amino quinazoline derivative with Keap1-Nrf2 pathway activation activity. LMDP10 binds to Keap1 to inhibit Keap1-Nrf2 interaction, thereby activating the Nrf2 pathway. LMDP10 elevates Nrf2, SOD, and GSH levels, reduces MDA and TNF-α levels, attenuates neurodegeneration, and improves memory function in Alzheimer’s disease (AD) rats. LMDP10 can be used for the study of AD.
    LMDP10
  • HY-N11722
    Panduratin A
    		Activator 99.9%
    Panduratin A is an orally active natural compound with multiple pharmacological activities. By specifically inhibiting the NF-κB signaling pathway, Panduratin A exerts potent anti-inflammatory and antioxidant effects in intestinal and vascular inflammation models. Panduratin A exerts a definite protective effect against Colistin (HY-113678)-induced nephrotoxicity by alleviating oxidative stress, improving mitochondrial dysfunction and inhibiting cell apoptosis. Panduratin A activates autophagy via an AMPK-dependent pathway and exhibits anti-tuberculosis activity. Panduratin A exerts antiviral effects by inhibiting the methyltransferase (DNA Methyltransferase) of SARS-CoV-2.
    Panduratin A
  • HY-B0298AS
    Clemastine-d5 fumarate
    		Activator 99.48%
    Clemastine (HS-592; Meclastine)-d5 fumarate is the deuterium labeled Clemastine fumarate. Clemastine fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
    Clemastine-d<sub>5</sub> fumarate
  • HY-N10405
    (R)-5-Hydroxy-1,7-diphenyl-3-heptanone
    		Activator 99.74%
    (R)-5-Hydroxy-1,7-diphenyl-3-heptanone is a diarylheptanoid that can be found in Alpinia officinarum. (R)-5-Hydroxy-1,7-diphenyl-3-heptanone ameliorates oxidative stress and insulin resistance via activation of Nrf2/ARE pathway.
    (R)-5-Hydroxy-1,7-diphenyl-3-heptanone
  • 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-N7088R
    Raffinose (Standard)
    		Activator
    Raffinose (Standard) is the analytical standard of Raffinose. This product is intended for research and analytical applications. Raffinose (Melitose) regulates intestinal flora, inhibits TLR4-MyD88-NF-κB signaling pathway, and activates Nrf2 signaling pathway. Raffinose exhibits anti-inflammatory, antioxidant, and immunomodulatory activities. Raffinose is orally active.
    Raffinose (Standard)
  • HY-17363S
    Dimethyl fumarate-d6
    		Activator 99.9%
    Dimethyl fumarate-d6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
    Dimethyl fumarate-d<sub>6</sub>
  • HY-N0509R
    Astilbin (Standard)
    		Activator
    Astilbin (Standard) is the analytical standard of Astilbin. This product is intended for research and analytical applications. Astilbin is a flavonoid compound and enhances NRF2 activation. Astilbin also suppresses TNF-α expression and NF-κB activation.
    Astilbin (Standard)
  • HY-136059
    Desfluoro-ezetimibe
    		Activator 99.54%
    Desfluoro-ezetimibe is a desfluoro impurity of Ezetimibe. Ezetimibe is a potent, metabolically stable cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
    Desfluoro-ezetimibe
  • HY-17376S1
    Ezetimibe-d4-1
    		Activator 99.26%
    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-N0527R
    Pentagalloylglucose (Standard)
    		Activator
    Pentagalloylglucose (Standard) is the analytical standard of Pentagalloylglucose. This product is intended for research and analytical applications. Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloylglucose inhibits UBE2T-mediated p53 ubiquitination, upregulates p53, downregulates RRM1/RRM2 in pancreatic cancer organoids. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities.
    Pentagalloylglucose (Standard)
  • HY-N3260
    Methyllucidone
    		Activator 98.0%
    Methyllucidone is a neuroprotective agent and an antioxidant that can be isolated from Lindera erythrocarpa Makino. Methyllucidone inhibits the ROS production, and activates antioxidant signaling pathways that include Nrf-2 and PI3K.
    Methyllucidone
Cat. No. Product Name / Synonyms Application Reactivity