Keap1-Nrf2-IN-30
Keap1-Nrf2-IN-30 is an orally active, blood-brain barrier-permeable Keap1-Nrf2 protein-protein interaction inhibitor with a Keap1 Kd value of 157 nM. Keap1-Nrf2-IN-30 selectively inhibits the Keap1-Nrf2 protein-protein interaction, promotes Nrf2 nuclear translocation, suppresses induced ferroptosis, reduces the expression of Aβ and p-Tau, and upregulates the expression of GPX4 and SLC7A11. Keap1-Nrf2-IN-30 upregulates the expression of HO-1 and NQO1, alleviates neuronal damage, and improves cognitive and spatial memory deficits. Keap1-Nrf2-IN-30 can be used in the research of Alzheimer's disease.
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- Formule: C38H47N6O11PS2
- Masse moléculaire:858.92
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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HO-1 |
NQO1 |
Keap1-Nrf2-IN-30 (compound 4-95) binds directly to purified Keap1 protein, with a KD value of 157 nM[1].
Keap1-Nrf2-IN-30 (8-32 μM; 8 h) dose-dependently restores the viability of HT-22 and SH-SY5Y cells undergoing ferroptosis induced by RSL-3 (HY-100218A) and Erastin (HY-15763)[1].
Keap1-Nrf2-IN-30 (32 μM) protects SH-SY5Y cells against Erastin-induced ferroptosis and lipid peroxidation in a Keap1-Nrf2-GPX4 axis-dependent manner, as knockdown of Keap1 or GPX4 abolishes its protective effect[1].
Keap1-Nrf2-IN-30 (32 μM) upregulates the protein expression of SLC7A11 and GPX4 in Erastin-induced ferroptotic SH-SY5Y cells in a Keap1-dependent manner, as Keap1 knockdown abolishes its effect[1].
Keap1-Nrf2-IN-30 (8-32 μM) dose-dependently restores GSH levels and reduces MDA levels and lipid peroxidation levels in HT-22 and SH-SY5Y cells undergoing Erastin-induced ferroptosis; it also inhibits ferroptotic morphological changes, cell death and mitochondrial damage[1].
Keap1-Nrf2-IN-30 (8-32 μM) upregulates the protein expression of GPX4 and SLC7A11 in a dose-dependent manner in Aβ1-42-treated SH-SY5Y cells, reduces Aβ accumulation and excessive phosphorylation of Tau; it activates the Keap1-Nrf2 pathway in a dose-dependent manner in Aβ1-42-treated SH-SY5Y cells by promoting Nrf2 nuclear translocation and upregulating downstream targets HO-1 and NQO1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT-22, SH-SY5Y neuronal cells
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Concentration:8, 16, 32 μM
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Incubation Time:8 h
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Result:Restored the viability of HT-22 and SH-SY5Y cells undergoing ferroptosis induced by RSL-3 (HY-100218A) and Erastin (HY-15763).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 6-8 weeks old, bilateral stereotaxic injection of Aβ1-42 oligomers into hippocampus)[1]
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Dosage:10 mg/kg; 20 mg/kg; 40 mg/kg
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Administration:i.g.; daily; 30 days
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Result:Raised elevated plus maze open-arm time dose-dependently; 40 mg/kg matched donepezil efficacy.
Boosted open-field central stay dose-dependently, total distance unchanged.
Improved novel object discrimination at 20/40 mg/kg to rescue recognition memory.
Restored spatial memory at 20/40 mg/kg via more platform crossings, shorter escape latency.
Dose-dependently upregulated hippocampal GPX4, SLC7A11 at 20/40 mg/kg.
Cut Aβ and p-Tau/Tau in hippocampus and cortex at 20/40 mg/kg.
Reduced hippocampal MDA, elevated GSH dose-dependently.
Increased Nrf2/HO-1/NQO1 and Nrf2 nuclear import, Keap1 unaltered.
Mitigated hippocampal neuronal damage at 40 mg/kg.
Chemical Information
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Masse moléculaire 858.92
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Formule C38H47N6O11PS2
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SMILES
O=S(N(CC(N)=O)C1=CC=C(N(CC(N)=O)S(=O)(C2=CC=C(NC([C@H]3CCCN3CCP(OCC)(COC)=O)=O)C=C2)=O)C4=CC=CC=C41)(C5=CC=C(OC)C=C5)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keap1-Nrf2-IN-30 Related Classifications
HY-184761 Related Classifications
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