1. Vías de señalización
  2. NF-κB
  3. Keap1-Nrf2

Keap1-Nrf2

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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-W016969
    2-Undecanone
    Activator 99.90%
    2-Undecanone is an orally active organic ketone. 2-Undecanone exerts antibacterial effects by inhibiting bacterial chaperone systems and interfering with the refolding of heat-inactivated proteins. 2-Undecanone also ameliorates asthmatic inflammation and airway remodeling by blocking the NF-κB pathway, and activates the Nrf2 pathway to reduce oxidative damage and prevent lung cancer induced by Benzo[a]pyrene (HY-107377). 2-Undecanone can be used in research related to cancer, asthma and infections.
    2-Undecanone
  • HY-N1902S
    4-Hydroxyphenylacetic acid-d6
    Activator 99.16%
    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.
    4-Hydroxyphenylacetic acid-d<sub>6</sub>
  • HY-N0394R
    L-Cystine (Standard)
    Activator
    L-Cystine (Standard) is the analytical standard of L-Cystine. This product is intended for research and analytical applications. L-Cystine, the extracellular form of L-Cysteine (HY-Y0337), is a nutritionally dispensable semiessential sulfur-containing amino acid, occurring in proteins of plants and animals. L-Cystine induces Nrf2 protein elevation in a Keap1 (HY-P75897)-dependent manner and activates Nrf2 transcription factor. L-cystine can elicit cytoprotection by reducing ROS generation and protecting against oxidant- or doxorubicin-induced apoptosis. The reduced reabsorption of L-Cystine in renal tubules and its poor solubility in urine are the important causes of cystine precipitation and cystine crystal formation eventually leading to kidney stones. L-Cystine combined with L-theanine (HY-15121) enhances the production of antigen-specific IgG by increasing glutathione (GSH) levels and T helper 2 (Th2) mediated responses in mice. L-Cystine is promising for research of cystinuria and cystinosis
    L-Cystine (Standard)
  • HY-119678
    Fortunellin
    Activator 98.31%
    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-112671
    CDDO-dhTFEA
    Activator 99.64%
    CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB. CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats.
    CDDO-dhTFEA
  • HY-B0854
    Mancozeb
    Activator
    Mancozeb is a widely used fungicide that is effective against fungal diseases in most cereals, vegetables, fruits and ornamental plants. In addition, Mancozeb can cause liver damage in mice by activating the Keap1/Nrf2 signaling pathway. Mancozeb upregulates lactate dehydrogenase and cytochrome c to alter cell metabolism and induce cell death. Mancozeb has reproductive toxicity and can induce apoptosis in ovarian cells.
    Mancozeb
  • HY-144634
    DDO-7263
    Activator 99.83%
    DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2-ARE activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 induces Nrf2 translocation into the nucleus. DDO-7263 inhibits of NLRP3 inflammasome activation. DDO-7263 exerts anti-inflammatory activity and has the potential for neurodegenerative diseases research, such as Parkinson's disease (PD).
    DDO-7263
  • HY-N0106
    (Rac)-Salvianic acid A sodium
    Activator 98.0%
    (Rac)-Salvianic acid A sodium is the racemic form of Salvianic acid A (HY-N1913). Salvianic acid A is an orally active phenolic compound that induces Nrf2/HO-1 activation and inhibits the NF-κB pathway, and it also activates the mitochondrial antioxidant defense system (Mitochondrial Metabolism). Salvianic acid A exhibits anti-inflammatory, antioxidant, and anti-apoptotic properties (Apoptosis), demonstrating potential for research into inflammation and cardiovascular diseases.
    (Rac)-Salvianic acid A sodium
  • HY-N4285
    Negletein
    Activator 99.55%
    Negletein (5,6-Dihydroxy-7-methoxyflavone) is a flavone found in Scutellaria. Negletein shows anti-inflammatory activity via inhibiting TNF-α and IL-1β with IC50 values of 16.4 and 6.4 μM, respectively. Negletein can activate Nrf2 and inhibit ROS production. Negletein can enhance the neuroprotective effect of nerve growth factor. Negletein can inhibit amyloid beta-peptide release and accumulation. Negletein can inhibit pathogens biofilms formation. Negletein can be used for the researches of cancer, infection, inflammation and neurological disease, such as colon cancer and Alzheimer's disease.
    Negletein
  • HY-W072025
    CYP2E1-IN-1
    Activator 99.95%
    CYP2E1-IN-1 (Compound 10) is an orally active cytochrome P450 2E1 (CYP2E1) inhibitor with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. CYP2E1-IN-1 activates the Nrf2/HO-1 signaling pathway and inhibits ROS production, thereby alleviating pancreatic injury. CYP2E1-IN-1 has significant anti-inflammatory and antioxidant activities and can effectively reduce inflammation and oxidative stress in severe acute pancreatitis (SAP). CYP2E1-IN-1 can be used in the study of SAP and other inflammatory-related diseases.
    CYP2E1-IN-1
  • HY-16561S
    Resveratrol-d4
    Activator 99.9%
    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. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
    Resveratrol-d<sub>4</sub>
  • HY-145532
    S-Allylmercaptocysteine
    Activator
    S-allylmercaptocysteine, an organic sulfur compound extracted from garlic, has anti-inflammatory and anti-oxidative effects for various pulmonary diseases. S-allylmercaptocysteine achieves its anti-cancer effect through a variety of pathways such as inducing the apoptosis of cancer cells through the TGF-β signaling pathway, or reducing the NF-κB activity and up-regulating Nrf2 to achieve the effects of anti-inflammation and anti-oxidation.
    S-Allylmercaptocysteine
  • HY-W019696
    Monoethyl fumarate
    Activator 99.88%
    Monoethyl fumarate is the monoethyl ester form of Fumaric acid (HY-W015883). Monoethyl fumarate is the activator for Nrf2. Monoethyl fumarate is a kind of effective preservative and polymerization agent for macromolecular material.
    Monoethyl fumarate
  • HY-N0008
    Orcinol glucoside
    Activator 99.40%
    Orcinol glucoside is an orally active, blood-brain barrier permeable osteoblast proliferation promoter that targets the Nrf2/Keap1, mTOR and p38 signaling pathways. Orcinol glucoside promotes Nrf2 nuclear translocation, upregulates antioxidant enzyme levels, enhances the phosphorylation of mTOR and p70S6K, and inhibits the enzymatic activity of HAS2 as well as the nuclear translocation of GR. Orcinol glucoside also alleviates oxidative stress, inhibits autophagic flux, osteoclastogenesis and TGF-β1-induced M2 polarization, while reducing collagen deposition and effectively promoting the proliferation, differentiation and mineralization of osteoblasts. Orcinol glucoside also exhibits anti-pulmonary fibrosis, anxiolytic and antidepressant activities. Orcinol glucoside can be used in the research of senile and glucocorticoid-induced osteoporosis, idiopathic pulmonary fibrosis (IPF), anxiety and other related diseases.
    Orcinol glucoside
  • HY-N3847
    Eriodictyol-7-O-glucoside
    Activator 99.80%
    Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is an Nrf2 activator. Eriodictyol-7-O-glucoside exhibits significant scavenging effects on both hydroxyl radicals and superoxide anions, with IC50 values of 0.28 mM and 0.30 mM, respectively. Eriodictyol-7-O-glucoside increases the nuclear localization of Nrf2 and induces the expression of the Nrf2/ARE-dependent genes. Eriodictyol-7-O-glucoside provides protection against oxygen and glucose deprivation (OGD)-induced oxidative insult. Eriodictyol-7-O-glucoside demonstrates neuroprotective efficacy in a rat model of focal cerebral ischemia (MCAO). Eriodictyol-7-O-glucoside can be used for the study of stroke.
    Eriodictyol-7-O-glucoside
  • HY-N0005S
    Curcumin-d6
    Activator 99.78%
    Curcumin-d6 (Diferuloylmethane-d6 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d<sub>6</sub>
  • HY-125972
    zr17-2
    Activator 98.01%
    zr17-2 is a cold inducible RNA-binding protein (CIRBP) agonist. zr17-2 has anti-inflammatory and anti-oxidant and can be used for the study of myocardial infarction. zr17-2 is a hypothermia mimetic molecule that reduces oxidative stress-induced retinal cell death.
    zr17-2
  • 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-171705
    KMS99220
    Activator 99.48%
    KMS99220 is an orally active, blood-brain barrier-permeable activator of the Nrf2 inhibitory protein Keap-1. KMS99220 enhances the activity of AMPK, activates the Nrf2 signaling pathway, and reduces the phosphorylation of IκB, nuclear translocation of NFκB, as well as the phosphorylation levels of JNK, IKK and p38 MAPK via HO-1. KMS99220 binds to Keap1 to trigger the nuclear translocation of Nrf2, induces the expression of HO-1, NQO1, GCLC, GCLM and proteasome subunits; enhances proteasomal enzymatic activity; inhibits iNOS expression, nitric oxide production and IL-1β generation; attenuates microglial activation; reduces α-synuclein aggregation; and prevents dopaminergic neuron degeneration and motor dysfunction. KMS99220 prevents the degeneration of dopaminergic neurons in the substantia nigra, induces the expression of Nrf2 downstream target genes, and effectively ameliorates associated motor dysfunction in a mouse model of Parkinson's disease. KMS99220 is applicable to research related to Parkinson's disease.
    KMS99220
  • HY-N0568R
    Madecassoside (Standard)
    Activator
    Madecassoside (Standard) is the analytical standard of Madecassoside. This product is intended for research and analytical applications. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity[10]. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
    Madecassoside (Standard)
Cat. No. Nombre del producto / Synonyms Application Reactivity