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-17376S
    Ezetimibe-d4
    		98.84%
    Ezetimibe-d4 is the deuterium labeled Ezetimibe. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
    Ezetimibe-d<sub>4</sub>
  • HY-111659
    His-Pro
    		Activator
    His-Pro is a dipeptide consisting of histidyl and proline.
    His-Pro
  • 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-W303895
    Luteolin monohydrate
    		Inhibitor 99.01%
    Luteolin (monohydrate) is the monohydrate of Luteolin. Luteolin (Luteoline), a flavonoid, is also a potent Nrf2 inhibitor. Luteolin has anti-inflammatory and anticancer properties, induces apoptosis and cell cycle arrest in multiple human cancer cell lines, including non-small lung cancer cells, and inhibits cell metastasis and angiogenesis.
    Luteolin monohydrate
  • HY-N3004
    Cyperotundone
    		≥98.0%
    Cyperotundone is a sesquiterpene isolated from Nagarmotha (Cyperus rotundus).
    Cyperotundone
  • 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-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
  • 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
  • HY-100489R
    TBHQ (Standard)
    		Activator 99.86%
    TBHQ (Standard) is the analytical standard of TBHQ. This product is intended for research and analytical applications. TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
    TBHQ (Standard)
  • 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-144635
    Nrf2-ARE/hMAO-B/QR2 modulator 1
    		Inhibitor 98.44%
    Nrf2-ARE/hMAO-B/QR2 modulator 1 is a Resveratrol-based multitarget-directed ligands with IC50s of 8.05, 9.83 and 0.57 μM for hMAO-B, NRF2 and QR2. Nrf2-ARE/hMAO-B/QR2 modulator 1 has neuroprotection, decreasing ROS production in okadaic acid-treated mice hippocampal slices.
    Nrf2-ARE/hMAO-B/QR2 modulator 1
  • HY-143333
    Nrf2 activator-3
    		Activator 98.26%
    Nrf2 activator-3 is a potent Nrf2 activator. Nrf2 activator-3 is used for cerebral ischemic injury research.
    Nrf2 activator-3
  • HY-N0005S
    Curcumin-d6
    		Activator 98.00%
    Curcumin-d6is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase (HATs) and also shows inhibitory effects on NF-κB and MAPKs.
    Curcumin-d<sub>6</sub>
  • HY-122054
    BPK-29
    		99.4%
    BPK-29 is a specific ligand that disrupts the atypical orphan nuclear receptor NR0B1-protein (such RBM45 and SNW1) interactions by covalently modifying C274. BPK-29 impairs the anchorage-independent growth of KEAP1-mutant cancer cells.
    BPK-29
  • 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].
    Dimethyl fumarate-d<sub>2</sub>
  • HY-B1328S
    Pyridoxine-d5
    Pyridoxine-d5 (Pyridoxol-d5) is a deuterium labeled Pyridoxine (HY-B1328). Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine-d<sub>5</sub>
  • HY-147517
    Keap1-Nrf2-IN-9
    		Inhibitor 98.52%
    Keap1-Nrf2-IN-9 (compound 11) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 0.575 µM. Keap1-Nrf2-IN-9 increases the expression of Nrf2 target genes including heme oxygenase 1 (Hmox1), glutathione S-transferase P (GstP), and glutamate-cysteine ligase catalytic (Gclc) and modulatory (Gclm) subunits. Keap1-Nrf2-IN-9 shows not cytotoxic activity in ARPE19 cells.
    Keap1-Nrf2-IN-9
  • HY-17376R
    Ezetimibe (Standard)
    		Activator 99.90%
    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)
  • HY-151362
    Keap1-Nrf2-IN-14
    		Inhibitor
    Keap1-Nrf2-IN-14 (compound 20c) is a KEAP1-NRF2 inhibitor that effectively disrupts the KEAP1-NRF2 interaction (IC50=75 nM) with a Kd value of 24 nM for KEAP1. Keap1-Nrf2-IN-14 induces the expression of NRF2 target genes and enhances the downstream antioxidant and anti-inflammatory activities. Keap1-Nrf2-IN-14 can be used in the study of oxidative stress-related inflammation.
    Keap1-Nrf2-IN-14
  • HY-N11657
    Sanggenon A
    		Inhibitor
    Sanggenon A (Sanggenone A) exerts anti-inflammatory effects by regulating NF-κB and HO-1/Nrf2 signaling pathways in BV2 and RAW264.7 cells. Sanggenon A markedly inhibits the Lipopolysaccharide (LPS; HY-D1056)-induced production of nitric oxide.
    Sanggenon A
Cat. No. Product Name / Synonyms Application Reactivity