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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- No. CAS: 3105470-83-2
- Fòrmula: C15H9BrO4
- Peso molecular:333.13
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Almacenamiento:
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Actividad biológica
Descripciòn
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.
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Cell Line:PC12, PC12-siNrf2 and PC12-siNT cells
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Concentration:5, 10, 20, 50, 100 µM
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Incubation Time:24 h
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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.
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Cell Line:PC12 cells
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Concentration:5, 10, 20 µM
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Incubation Time:2, 4, 8 h
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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.
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Cell Line:PC12 cells
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Concentration:20 µM
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Incubation Time:6, 12, 24 h
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Result:Significantly upregulated HO-1, NQO1, Trx, TrxR, and GCLC mRNA after 6 h.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult AB-strain zebrafish (6-months old) challenged with SCA (200 μM in water)[1]
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Dosage:5 μM
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Administration:48 h
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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.
Chemical Information
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No. CAS 3105470-83-2
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Peso molecular 333.13
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Fòrmula C15H9BrO4
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SMILES
BrC(C=C1)=CC=C1C2=COC3=C(O)C(O)=CC=C3C2=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keap1/Nrf2/ARE activator 2 Related Classifications
HY-180155 Related Classifications
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