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-N3847
    Eriodictyol-7-O-glucoside
    		Activator 99.82%
    Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is a potent free radical scavenger. Eriodictyol-7-O-glucoside is also an Nrf2 activator, confers protection against Cisplatin-induced toxicity.
    Eriodictyol-7-O-glucoside
  • HY-162152
    biKEAP1
    		Inhibitor
    biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models.
    biKEAP1
  • HY-121523
    MIND4-17
    		Activator 99.93%
    MIND4-17 is a potent NRF2 activator that covalently modifies a C151 residue of Keap1. MIND4-17 disrupts Keap1-Nrf2 association, leading to Nrf2 protein stabilization and nuclear translocation. MIND4‐17 exerts potent antioxidant activity.
    MIND4-17
  • HY-N0682S3
    Pyridoxine-13C4 hydrochloride
    		98.00%
    Pyridoxine-13C4 (hydrochloride) is the 13C-labeled Pyridoxine (hydrochloride). Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine-<sup>13</sup>C<sub>4</sub> hydrochloride
  • HY-N0682S
    Pyridoxine-d3 hydrochloride
    		≥99.0%
    Pyridoxine-d3 (hydrochloride) is the deuterium labeled Pyridoxine hydrochloride. Pyridoxine hydrochloride (Pyridoxol; Vitamin B6) is a pyridine derivative. Pyridoxine (Pyridoxol; Vitamin B6) exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
    Pyridoxine-d<sub>3</sub> hydrochloride
  • HY-17363R
    Dimethyl fumarate (Standard)
    		Activator
    Dimethyl fumarate (Standard) is the analytical standard of Dimethyl fumarate. This product is intended for research and analytical applications. 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.
    Dimethyl fumarate (Standard)
  • HY-N6802
    Tigloylgomisin H
    		Inducer
    Tigloylgomisin H is a lignan isolated from the fruits of S. chinensis, can induce quinone reductase (QR) activity in Hepa1c1c7 mouse hepatocarcinoma cells. Tigloylgomisin H functions as a monofunctional inducer that specifically upregulates phase II detoxification enzyme NQO1 through the NF-E2-related factor 2 (Nrf2)-ARE pathway, thus represents a potential liver cancer prevention agent.
    Tigloylgomisin H
  • HY-RS16271
    Nrf-2 Mouse Pre-designed siRNA Set A
    		Inhibitor
    Nrf-2 Mouse Pre-designed siRNA Set A includes three pairs of siRNA designed for different regions of the Nrf-2 (Mouse) gene, along with a negative control, a FAM-labeled negative control, and a positive control.
    Nrf-2 Mouse Pre-designed siRNA Set A
    Nrf-2 Mouse Pre-designed siRNA Set A
  • 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.
    Antioxidant agent-20
  • HY-149244
    Nrf2 activator-7
    		Activator
    Nrf2 activator-7 (Compound 12b) is a potent Nrf2 activator and significantly activates the Nrf2 signaling pathway.
    Nrf2 activator-7
  • 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.
    Nrf2 activator-8
  • HY-161992
    Nrf2 activator-11
    		Activator
    Nrf2 activator-11 (compound M11) is a Nrf2 activator with blood-brain permeability. Nrf2 activator-11 has anti-oxidation, anti-inflammation, anti-ferroptosis and anti-apoptosis. Nrf2 activator-11 can be used to study cerebral  ischemia-reperfusion (CI/R) injury models.
    Nrf2 activator-11
  • HY-P5480
    Keap1-Nrf2-IN-16
    Keap1-Nrf2-IN-16 is a biological active peptide. (KEAP1 binding activity)
    Keap1-Nrf2-IN-16
  • HY-N0625AR
    Alpinetin (Standard)
    		Activator
    Alpinetin (Standard) is the analytical standard of Alpinetin. This product is intended for research and analytical applications. 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.
    Alpinetin (Standard)
  • HY-168161
    Keap1-Nrf2-IN-23
    		Inhibitor
    Keap1-Nrf2-IN-23 (compound 56) is an inhibitor of the Keap1–Nrf2 PPI (IC50=16.0 nM). Keap1-Nrf2-IN-23 binds to Keap1 with a Kd value of 3.07 nM. Keap1-Nrf2-IN-23 has oral activity.
    Keap1-Nrf2-IN-23
  • HY-160876
    BC-1901S
    		Activator
    BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury.
    BC-1901S
  • HY-N0807R
    Swertiamarin (Standard)
    		Modulator
    Swertiamarin (Standard) is the analytical standard of Swertiamarin. This product is intended for research and analytical applications. Swertiamarin is an orally active iridoid compound with hypoglycemic, hypolipidemic, anti rheumatic and antioxidant activities, which can be used in the research of diabetes and arthritis.
    Swertiamarin (Standard)
  • HY-N6641R
    Monascin (Standard)
    		Activator
    Monascin (Standard) is the analytical standard of Monascin. This product is intended for research and analytical applications. Monascin is a kind of azaphilonoid pigments extracted from Monascus pilosus-fermented rice (red-mold rice). Monascin also exhibits anti-tumor-initiating activity and anti-inflammatory activity with oral administration. Monascin inhibits the activation of NOR 1 (an NO donor). Monascin is a Nrf2 activator and PPARγ agonist.
    Monascin (Standard)
  • HY-157929
    Keap1-Nrf2-IN-19
    		Inhibitor
    Keap1-Nrf2-IN-19 (compound 33) is an oral active Keap1-Nrf2 protein–protein interaction (PPI) inhibitor with the Kd value of 0.0014 μM. Keap1-Nrf2-IN-19 exhibits less than 50% inhibition at 30 μM against hERG and 10 μM against CYPs.
    Keap1-Nrf2-IN-19
  • HY-155784
    SPC-180002
    		Activator
    SPC-180002 is a SIRT1/3 dual inhibitor, with IC50 values of 1.13 and 5.41 μM, respectively. SPC-180002 disturbs redox homeostasis via ROS generation, which leads to an increase in both p21 protein stability and mitochondrial dysfunction. SPC-180002 strongly inhibits cell cycle progression and cancer cell growth. SPC-180002 activates the Nrf2 signaling pathway.
    SPC-180002
Cat. No. Product Name / Synonyms Application Reactivity