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  3. Nrf2/HO-1 activator 2

Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD).

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Nrf2/HO-1 activator 2 Chemical Structure

Nrf2/HO-1 activator 2 Chemical Structure

CAS No. : 2883506-31-6

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Description

Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD)[1].

In Vitro

Nrf2/HO-1 activator 2 (compound 13m; 0.1-30 µM; 24 h) has protection to PC12 cells against toxicity and inhibits 6-OHDA- and Rotenone (HY-B1756)- induced cell death[1].
Nrf2/HO-1 activator 2 (1-100 µM; 11 h) inhibits 6-OHDA- or rotenone-induced production of reactive oxygen species and partially attenuates lipid peroxidation in rat brain homogenates. Nrf2/HO-1 activator 2 inhibits the production of lipid peroxide in rat brain homogenates by 28.8% at 100 μM[1].
Nrf2/HO-1 activator 2 (1-100 µM; 11 h) up-regulates heme oxygenase-1 (HO-1) and Nrf2 expression[1].
Nrf2/HO-1 activator 2 (10 µM; 2-3 h; PC12 cells) activator 2 activates Nrf2/HO-1 signaling by phosphorylated ERK1/2, JNK, and Akt[1].

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

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 3, 5, 7, 10 and 30 µM, 6-OHDA (50 µM); 0.1, 0.3, 1, 3, 10, and 30 µM, Rotenone (1 µM)
Incubation Time: 24 hours
Result: Exhibited neuroprotective effects on 6-OHDA-induced toxicity in dose-dependent manners.
Rescued cells from rotenone-induced damage, with increased levels of cell viability up to 79.9% at 30 μM.

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 0, 1, 3, 10, and 30 µM
Incubation Time: 24 hours
Result: Upregulated HO-1 levels in a dose-dependent manner, with 1.5- and 2-fold increases at 30 μM concentrations, respectively.
Enhanced the nuclear translocation of Nrf2 in PC12 cells after 3 h at 10 µM.

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 10 µM
Incubation Time: 2-3 hours
Result: Induced the phosphorylation of ERK1/2, JNK, and Akt.
Molecular Weight

374.33

Formula

C20H16F2O5

CAS No.
SMILES

O=C1C(C2=CC=C(F)C=C2F)=COC3=C1C4=C(CC(O)C(C)(C)O4)C(O)=C3

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Nrf2/HO-1 activator 2
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HY-151431
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