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-157928
    Keap1-Nrf2-IN-18
    		Inhibitor
    Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM).
    Keap1-Nrf2-IN-18
  • HY-Z0548R
    Methyl 3,4-dihydroxybenzoate (Standard)
    		Agonist
    Methyl 3,4-dihydroxybenzoate (Standard) is the analytical standard of Methyl 3,4-dihydroxybenzoate. This product is intended for research and analytical applications. Methyl 3,4-dihydroxybenzoate (Protocatechuic acid methyl ester; Methyl protocatechuate) is a major metabolite of antioxidant polyphenols found in green tea. Antioxidant and anti-inflammatory effect.
    Methyl 3,4-dihydroxybenzoate (Standard)
  • HY-N1902R
    4-Hydroxyphenylacetic acid (Standard)
    		Activator
    4-Hydroxyphenylacetic acid (Standard) is the analytical standard of 4-Hydroxyphenylacetic acid. This product is intended for research and analytical applications. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2. IC50 & Target:Nrf2 In Vivo: 4-Hydroxyphenylacetic acid (6, 12, or 25 mg/kg) increases Nrf2 translocation to the nucleus and enhances the activity of phase II and antioxidant enzymes. The protein levels of nuclear Nrf2 are increased by 170% and 230% in pre-treated 12 and 25 mg/kg 4-Hydroxyphenylacetic acid groups, respectively, compared with the control group.The 4-Hydroxyphenylacetic acid pretreatment at a final dose of 25 mg/kg markedly and selectively up-regulated the target genes of phase II enzymes and resulted in higher up-regulation than that of the control group by 270%, 400%, and 500% or UGT1A1, UGT1A9, and SULT2A1, respectively. 4-Hydroxyphenylacetic acid also suppresses the expression of CYP2E1.
    4-Hydroxyphenylacetic acid (Standard)
  • HY-N10405
    (R)-5-Hydroxy-1,7-diphenyl-3-heptanone
    		Activator 99.71%
    (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-163315
    YPLP
    YPLP is a yeast-derived peptide Tyr-Pro-Leu-Pro, which exhibits activity in anti fatigue mechanisms through the nuclear factor erythroid-2-related factor 2 (Nrf2)- and AMP-activated protein kinase (AMPK) pathway. YPLP is orally active.
    YPLP
  • HY-171035
    PRL-295
    		Inhibitor
    PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction。PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice.
    PRL-295
  • HY-156081
    Nrf2 activator-9
    		Activator
    Nrf2 activator-9 (compound D-36) is an Nrf2 activator that inhibits oxidized low-density lipoprotein (oxLDL) and high glucose (HG)-induced apoptosis in HUVEC cells. Nrf2 activator-9 inhibits oxLDL and HG-induced vascular endothelial cell (VEC) injury and can effectively prevent and treat atherosclerosis.
    Nrf2 activator-9
  • HY-17363S
    Dimethyl fumarate-d6
    		Activator 99.49%
    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[1][2][3][4][5][6].
    Dimethyl fumarate-d<sub>6</sub>
  • HY-169315
    Nrf2 activator 17
    		Activator
    Nrf2 activator 17 (compound 10) is an Nrf2 activator that inhibits the interaction between Keap1 and Nrf2 with an IC50 of < 0.1 pM. Additionally, Nrf2 activator 17 has an EC50 of < 10 μM in HepG2 cells.
    Nrf2 activator 17
  • HY-161783
    HDAC6-IN-45
    		Activator
    HDAC6-IN-45 (Compound 15) is a selective inhibitor for HDAC6 with IC50 of 15.2 nM. HDAC6-IN-45 exhibits neurotrophic through the upregulation of GAP43 and Beta-3 tubulin markers. HDAC6-IN-45 activates the Nrf2 signaling pathway, reduces H2O2-induced ROS production, inhibits apoptosis in PC12, and exhibits neuroprotective efficacy in SCOP-induced zebrafish Alzheimer's Disease models. HDAC6-IN-45 exhibits antioxidant activity and good blood-brain barrier (BBB) permeability.
    HDAC6-IN-45
  • HY-N1902S1
    4-Hydroxyphenylacetic acid-d4
    4-Hydroxyphenylacetic acid-d4 is the deuterium labeled 4-Hydroxyphenylacetic acid[1]. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2[2].
    4-Hydroxyphenylacetic acid-d<sub>4</sub>
  • HY-N6953R
    Garcinone D (Standard)
    		Activator
    Garcinone D (Standard) is the analytical standard of Garcinone D. This product is intended for research and analytical applications. Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration-and time-dependent manners.
    Garcinone D (Standard)
  • HY-161643
    S21-1011
    		Activator
    S21-1011 is a selective inhibitor for butyrylcholinesterase (BChE), with IC50 of 0.059 and 0.162 μM, for eqBChE and hBChE, respectively. S21-1011 exhibits good blood-brain barrier (BBB) permeability and good pharmacokinetic characters. S21-1011 exhibits anti-inflammatory activity through activation of keap1-Nrf2-ARE pathway (EC50 is 23.48 μM for antioxidant element ARE activation), ameliorates cognitive impairment in murine Alzheimer’s disease model.
    S21-1011
  • 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-152037
    AChE/Nrf2 modulator 1
    		Modulator
    AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease.
    AChE/Nrf2 modulator 1
  • HY-P10530
    Nrf2 (69-84)
    Nrf2 (69-84) is a peptide fragment of Nrf2 protein that contains the key ETGE motif, which is an important region for binding to the Kelch domain of Keap1 protein. Nrf2 (69-84) can be used to study the role of Nrf2 in the development and progression of diseases, especially in cancer, neurodegenerative diseases and inflammatory diseases.
    Nrf2 (69-84)
  • HY-N10431
    Stigmane B
    		Activator
    Stigmane B (Compound 2) is a nuclear factor E2-related factor (Nrf2) activator. Stigmane B downregulates apoptosis and reactive oxygen species (ROS) generation, and increases antioxidant enzyme activities. Stigmane B shows neuroprotective effects.
    Stigmane B
  • HY-153873
    MSU38225
    		Inhibitor 99.52%
    MSU38225 is an Nrf-2 inhibitor that increases levels of reactive oxygen species (ROS). MSU38225 inhibits the growth of human lung cancer cells and enhances the sensitivity of human lung cancer cells to chemotherapy in vitro and in vivo. MSU38225 can be used in cancer research.
    MSU38225
  • HY-143893
    Keap1-Nrf2-IN-6
    		Inhibitor
    Keap1-Nrf2-IN-6 (compound 64) is a potent and selective Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with an IC50 of 41 nM, Kd of 68 nM.
    Keap1-Nrf2-IN-6
  • HY-N0512R
    Loganin (Standard)
    		Activator
    Loganin (Standard) is the analytical standard of Loganin. This product is intended for research and analytical applications. Loganin is a type of iridoid glycoside compound that possesses anti-inflammatory, antioxidant, and antitumor properties, and offers protective effects against acute lung injury and pulmonary fibrosis. Loganin exerts its protective effects against LPS (HY-D1056)-mediated inflammation and oxidative stress by upregulating the Nrf2/HO-1 signaling pathway, and it reduces neuroinflammation caused by spinal cord injury (SCI).
    Loganin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity