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.

Keap1-Nrf2 Related Products (296):

Cat. No. Product Name Effect Purity
  • HY-100523
    ML385 Inhibitor 99.96%
    ML385 is a specific nuclear factor erythroid 2-related factor 2 (NRF2) inhibitor with an IC50 of 1.9 μM.
  • HY-112675
    4-Octyl itaconate Activator 99.92%
    4-Octyl Itaconate is a cell-permeable Itaconate derivative. Itaconate is an anti-inflammatory metabolite that activates Nrf2 via alkylation of KEAP1[1].
  • HY-N0162
    Luteolin Inhibitor 99.51%
    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[1][2][3].
  • HY-16561
    Resveratrol Activator
    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].
  • HY-N0005
    Curcumin Activator 98.84%
    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 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.
  • HY-173307
    Nrf2 activator 19 Activator
    Nrf2 activator 19 is a BBB-penetrable NRF2/HO-1 activator. Nrf2 activator 19 exerts potent antioxidant and neuroprotective effects. Nrf2 activator 19 can also effectively reduce brain damage, reduce Reactive Oxygen Species (ROS) accumulation. Nrf2 activator 19 inhibits neuronal apoptosis. Nrf2 activator 19 promotes the recovery of neurological function and motor ability. Nrf2 activator 19 shows significant potential in ischemic stroke research[1].
  • HY-173187
    Keap1-Nrf2-IN-27 Inhibitor
    Keap1-Nrf2-IN-27 (compound 1C) is a inhibitor of Keap1-Nrf2 protein-protein interaction (PPI) with KD2 value of 0.119 μM. Keap1-Nrf2-IN-27 suppresses the expression of pro-inflammatory cytokine TNF-α and IL-6 in the LPS-induced RAW264.7 cell model[1].
  • HY-173181
    Anticonvulsant agent 10 Inhibitor
    Anticonvulsant agent 10 (Compound 6d) is an inhibitor targeting the Keap1-Nrf2 interaction, with a potent ED50 of 0.04 mmol/kg. By inhibiting Keap1-Nrf2 binding and activating the Nrf2/ARE pathway, Anticonvulsant agent 10 exerts anticonvulsant and neuroprotective effects, making it suitable for research in antiepileptic and neuroprotective studies[1].
  • HY-N0818
    Chikusetsusaponin Iva Inhibitor
    Chikusetsusaponin IVa is an orally active protein kinase activator. Chikusetsusaponin IVa binds to YAP with a KD value of 0.388 mM. Chikusetsusaponin IVa reduces inflammatory mediators (IL-6, IL-10, COX-2) expression, NO production, promotes ROS generation, induces Apoptosis, inhibits MAPK, TAZ, and regulates Nrf2, JAK/STAT. Chikusetsusaponin Iva has anti-H9N2 AIV and anti-endometrial cancer activities. Chikusetsusaponin Iva shows anti-inflammatory, hepatoprotective and osteoprotective effects[1][2][3][4][5][6][7][8][9][10].
  • HY-N1970R
    5,7-Dihydroxychromone (Standard) Activator
    5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone. This product is intended for research and analytical applications. 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[1].
  • HY-170579
    Antioxidant agent-20 Activator
    Antioxidant agent-20 (Compound 3d) has potent anti-inflammatory and antioxidant activity. Antioxidant agent-20 reduces reactive oxygen species (ROS) and apoptosis in a dose-dependent manner. Antioxidant agent-20 exhibits photoprotective effect against UVB-irradiated human skin keratinocytes (HaCaT) (IC50=5.13 µM) via activation of Nrf2/HO-1 signaling and inhibition of NF-κB pathway[1].
  • HY-149244
    Nrf2 activator-7 Activator
    Nrf2 activator-7 (Compound 12b) is a potent Nrf2 activator and significantly activates the Nrf2 signaling pathway.
  • HY-N1914
    Ergothioneine Inhibitor
    Ergothioneine is an imidazole-2-thione derivative with orally active histidine betaine. Ergothioneine is a specific inhibitor of p38-MAPK and Akt, which plays a protective role in cell apoptosis induced by stress. Ergothioneine has antioxidant activity[1][2].
  • HY-N0625A
    Alpinetin Activator 99.51%
    Alpinetin is a flavonoid isolated from cardamom and possesses antitumor, antiinflammation, hepatoprotective, cardiovascular protective, lung protective, antibacterial, antiviral, neuroprotective properties. Alpinetin inhibits lipopolysaccharide (LPS)-induced inflammation, activates PPAR-γ, activates Nrf2, and inhibits TLR4 expression to protect LPS-induced renal injury[1][2][3][4].
  • HY-170887
    MAO-B-IN-39 Inducer
    MAO-B-IN-39 (compound11) is a selective monoamine oxidase B (MAO-B) inhibitor. MAO-B-IN-39 inhibits MAO-Bwith an IC50 of 3.61 μM. MAO-B-IN-39 demonstrates a potent NRF2 induction capacity. MAO-B-IN-39 exhibits potent anti-inflammatory and neuroprotective activity in OS (oxidative stress)-related in vitro models. MAO-B-IN-39 demonstrates high liver microsomal stability and favorable pharmacokinetics in mice. MAO-B-IN-39 is potential for Parkinson’s disease (PD) research[1].
  • HY-17363S1
    Dimethyl fumarate-d2 99.20%
    Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate[1]. 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[2][3].
  • HY-101140
    KI696 Inhibitor
    KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction[1].
  • HY-W009731
    Dibenzoylmethane Activator
    Dibenzoylmethane, a minor ingredient in licorice, activates Nrf2 and prevents various cancers and oxidative damage. Dibenzoylmethane, an analog of curcumin, results in dissociation from Keap1 and nuclear translocation of Nrf2[1].
  • HY-N3075
    Phytol Inhibitor
    Phytol ((E)-Phytol) is an orally active diterpenoid alcohol that can be extracted from chlorophyll. Phytol has antioxidant, anti-inflammatory, anti-schistosomiasis and antibacterial activities[1][2][3].
  • HY-155572
    Nrf2 activator-8 Activator
    Nrf2 activator-8 (compound 10e) is a Nrf2 activator (EC50=37.9 nM). Nrf2 activator-8 exhibits remarkable antioxidant and anti-inflammatory effects in BV-2 microglial cells. Nrf2 activator-8 can significantly restore spatial memory deficits in a mouse model of lipopolysaccharide (LPS)-induced neuroinflammation[1].