Keap1-Nrf2-IN-31
Keap1-Nrf2-IN-31 is a potent Keap1-Nrf2 interaction (PPI) inhibitor. Keap1-Nrf2-IN-31 binds with dual high affinity to the KDC (Kd = 1.2 μM (MST assay); Kd = 171 nM (SRP assay)) and BTB (Kd = 71 nM (MST assay); Kd = 74.1 nM (SRP assay)) domains of Keap1, inhibits the function of the Keap1-Cul3 complex and blocks the ubiquitination-mediated degradation of Nrf2, thereby promoting Nrf2 nuclear translocation and activating the expression of antioxidant genes. Keap1-Nrf2-IN-31 can be used for research on Parkinson's disease.
For research use only. We do not sell to patients.
- CAS No.: 152243-63-5
- Formula: C27H36O7
- Molecular Weight:472.57
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Storage:
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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Biological Activity
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Chemical Information
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Biological Activity
Description
IC50 & Target
[1]|
Caspase-3 |
NQO1 |
β3-tubulin |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SH-SY5Y | EC50 |
100 nM
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Protection against rotenone-induced toxicity in human neuroblastoma SH-SY5Y cells assessed as cell viability.
Protection against rotenone-induced toxicity in human neuroblastoma SH-SY5Y cells assessed as cell viability.
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acsmedchemlett.6c00156 |
In Vitro
Keap1-Nrf2-IN-31 (compound 4a) (100 nM; 24 h) upregulates tyrosine hydroxylase (TH) and β3-tubulin protein expression and inhibits Cleaved caspase 3 expression in Rotenone (HY-B1756)-induced SH-SY5Y cells[1].
Keap1-Nrf2-IN-31 (100 nM; 24 h) increases HO-1, GCLC, and NQO1 mRNA expression levels in Rotenone-exposed SH-SY5Y cells, increases NQO1 and GCLC protein expression, and promotes Nrf2 nuclear translocation[1].
Keap1-Nrf2-IN-31 binds Keap1 BTB with a KD of 1.2 μM and KDC with a KD of 71 nM in MST assays[1].
Keap1-Nrf2-IN-31 is a high-affinity Keap1 binder, with a KD of 171 nM for BTB and a KD of 74.1 nM for KDC as measured by SPR, and it binds site-specifically at the Nrf2 site[1].
Keap1-Nrf2-IN-31 (10-1000 nM; 24 h) protects SH-SY5Y cells against Rotenone (HY-B1756)-induced toxicity, with a maximal effect and an EC50 of 100 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:10, 100, 500, 1000 nM
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Incubation Time:24 h
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Result:Provided significant neuroprotection against rotenone-induced toxicity, showing maximum protection at 100 nM and demonstrating an EC50 of 100 nM.
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Cell Line:SH-SY5Y cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Significantly increased the mRNA expression levels of Nrf2 downstream antioxidant enzymes HO-1, NQO1, and GCLC.
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Cell Line:SH-SY5Y cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Restored the protein levels of tyrosine hydroxylase (TH) and β3-tubulin, inhibited the expression of Cleaved caspase 3, and enhanced the protein levels of GCLC, NQO1, and nuclear Nrf2.
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Cell Line:SH-SY5Y cells
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Concentration:100 nM
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Incubation Time:24 h
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Result:Significantly ameliorated the rotenone-induced decrease in tyrosine hydroxylase (TH) signals in dopaminergic neurons
Chemical Information
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CAS No. 152243-63-5
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Molecular Weight 472.57
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Formula C27H36O7
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SMILES
CC(C=C1)=CC2=C1C(C)(C)OC3=C2C(O[C@@H]4O[C@H](CO)[C@@H](O)[C@H](O)[C@H]4O)=CC(CCCCC)=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keap1-Nrf2-IN-31 Related Classifications
HY-189812 Related Classifications
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Keywords
- Keap1-Nrf2-IN-31
- 152243-63-5
- Keap1-Nrf2
- Quinone Reductase
- Tyrosine Hydroxylase
- Microtubule/Tubulin
- Caspase
- BTB domain
- KDC domain
- Keap1-Cul3 interaction
- Keap1-Nrf2 interaction
- Nrf2 nuclear translocation
- Parkinson's disease
- antioxidant enzyme
- dopaminergic neurons
- neuroblastoma cell model
- rotenone-induced apoptosis
- Inhibitor
- inhibitor
- inhibit