2. NF-κB Neuronal Signaling Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease
  3. Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase
  4. Keap1/Nrf2/ARE activator 2

Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease.

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Keap1/Nrf2/ARE activator 2

Keap1/Nrf2/ARE activator 2 Chemical Structure

CAS No. : 3105470-83-2

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Keap1/Nrf2/ARE activator 2 Related Antibodies

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HO-1 HO-2

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Description

Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

IL-6

 

IL-1β

 

AChE

14.79 μM (IC50)

AChE

1.35 μM (Ki)

HO-1

 

NQO1

 

In Vitro

Keap1/Nrf2/ARE activator 2 (compound 32) (5-100 µM, 24 h) demonstrates no significant toxic effect on PC12 cells upto 20 μM[1].
Keap1/Nrf2/ARE activator 2 (5-20 µM, 12-24 h) demonstrates significant cytoprotection against H2O2- and SCA-induced PC12 cell injury, as evidenced by improved cell viability, reduced LDH and ROS release, and suppression of apoptosis[1].
Keap1/Nrf2/ARE activator 2 (20 µM, 2-8 h) induces Nrf2 accumulation and nuclear translocation in PC12 cells in a time-dependent manner[1].
Keap1/Nrf2/ARE activator 2 (20 µM, 6-24 h) upregulates multiple antioxidant systems in PC12 cells, such as HO-1, NQO1, Trx, TrxR, and GCLC mRNA[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Keap1/Nrf2/ARE activator 2 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC12, PC12-siNrf2 and PC12-siNT cells
Concentration: 5, 10, 20, 50, 100 µM
Incubation Time: 24 h
Result: Displayed no significant toxic effect on PC12 cells upto 20 μM following 24 h exposure.
Rescued PC12 cells from the H2O2-induced oxidative damages.
Demonstrated robust protection against SCA-induced cytotoxicity.
Significantly protected the control cells from the H2O2-induced injury, while showing no protective effect in the Nrf2-deficient cells.
Showed a protective effect in PC12-siNrf2 cells.

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 5, 10, 20 µM
Incubation Time: 2, 4, 8 h
Result: Significantly activated the Nrf2/ARE signaling pathway.
Showed a marked increase in total and nuclear Nrf2 levels as early as 2 h after treatment.

Real Time qPCR[1]

Cell Line: PC12 cells
Concentration: 20 µM
Incubation Time: 6, 12, 24 h
Result: Significantly upregulated HO-1, NQO1, Trx, TrxR, and GCLC mRNA after 6 h.
In Vivo

Keap1/Nrf2/ARE activator 2 (5 μM, 48 h) ameliorates SCA-induced cognitive impairment in zebrafish by reducing neuroinflammation, restoring cholinergic function, and activating the Nrf2/ARE antioxidant pathway[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Adult AB-strain zebrafish (6-months old) challenged with SCA (200 μM in water)[1]
Dosage: 5 μM
Administration: 48 h
Result: Significantly improved spatial memory performance in zebrafish challenged with scopolamine, as evidenced by increased preference for the target arm in the T-maze test and enhanced orientation.
Restored swimming velocities, suggesting improved motor function.
Reduced neuroinflammation by attenuating the expression of IL-1β, IL-6, TNF-α and upregulated the expression of antioxidant genes (Nrf2, Gpx4, Trx).
Restored AChE activity to near-physiological levels.
Molecular Weight

333.13

Formula

C15H9BrO4
CAS No.
SMILES

BrC(C=C1)=CC=C1C2=COC3=C(O)C(O)=CC=C3C2=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Keap1/Nrf2/ARE activator 2 Related Classifications

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Keywords:

Keap1/Nrf2/ARE activator 23105470-83-2Keap1-Nrf2Cholinesterase (ChE)Interleukin RelatedTNF ReceptorReactive Oxygen Species (ROS)Heme Oxygenase (HO)Quinone ReductaseILTumor Necrosis Factor ReceptorTNFRHeme OxygenaseAChEOxidative stressNrf2NeuroprotectionInhibitorinhibitorinhibit

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