Keap1-Nrf2 PPI-IN-2
Keap1-Nrf2 PPI-IN-2 is a Keap1-Nrf2 PPI inhibitor with an EC50 of 14.2 μM. Keap1-Nrf2 PPI-IN-2 covalently binds to Keap1 cysteine residues through its electrophilic itaconate moiety, disrupts the Keap1-Nrf2 protein-protein interaction, releases Nrf2, and promotes its nuclear translocation and antioxidant gene expression, thereby reducing ROS and inhibiting IL-13 production. Keap1-Nrf2 PPI-IN-2 can be used for research on atopic dermatitis.
For research use only. We do not sell to patients.
- Formula: C50H38F10IrN8O3P
- Molecular Weight:1212.06
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Keap1 0.627 μM (Kd) |
IL-13 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
8.7 μM
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Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42720490 |
| HUVEC | IC50 |
> 10 μM
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Cytotoxicity against human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human HUVEC cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42720490 |
| HaCaT | IC50 |
> 10 μM
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Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human HaCaT cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42720490 |
| A-375 | IC50 |
9.95 μM
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Cytotoxicity against human A375 skin cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Cytotoxicity against human A375 skin cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
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42720490 |
In Vitro
Keap1-Nrf2 PPI-IN-2 (8 h) modulates ROS levels in HaCaT cells[1].
Keap1-Nrf2 PPI-IN-2 (20 μM; 0.5 h) binds to Keap1 in HaCaT cell lysates[1].
Keap1-Nrf2 PPI-IN-2 (150 μM; 25 °C) binds to Keap1 with a Kd of 0.627 μM and a stoichiometry of approximately 2:1[1].
Keap1-Nrf2 PPI-IN-2 inhibits the Keap1-Nrf2 PPI with an EC50 of 14.2 μM[1].
Keap1-Nrf2 PPI-IN-2 (10 μM; 2 h) mainly localizes in the cytoplasm of HaCaT cells[1].
Keap1-Nrf2 PPI-IN-2 (10 μM; 1.5-2.5 h) effectively enters HaCaT cells[1].
Keap1-Nrf2 PPI-IN-2 (10 μM) effectively stimulates ARE transcriptional activity in HaCaT cells[1].
Keap1-Nrf2 PPI-IN-2 (72 h) exhibits specific cytotoxic profiles against HaCaT, LO2, HUVEC, and HEK293T cell lines in the MTT assay[1].
Keap1-Nrf2 PPI-IN-2 (10 µM; 8 h) activates ARE-luciferase activity in HaCaT cells[1].
Keap1-Nrf2 PPI-IN-2 (10-20 μM; 2 h) exhibits luminescence in HaCaT and A375 cells after 2 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT
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Concentration:20 μM
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Incubation Time:0.5 h
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Result:Significantly stabilized Keap1 even at high temperatures up to 70 °C.
No significant stabilized effect was observed for Nrf2.
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Cell Line:HaCaT
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Concentration:10 μM
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Incubation Time:2 h
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Result:Mainly accumulated in the cytoplasm.
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Cell Line:HaCaT
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Concentration:1, 3, and 10 μM
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Incubation Time:8 h
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Result:Induced NQO1 and HO-1 protein levels in a dose-dependent manner.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, DNFB-induced)[1]
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Dosage:5; 15 mg/kg
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Administration:topical; once daily; 12 consecutive days
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Result:Caused milder body weight loss than dexamethasone.
Showed significantly lower AD lesion severity than the DNFB model group.
Relieved pruritus notably after 4 days.
Markedly reversed DNFB-induced serum IgE elevation.
Ameliorated DNFB-triggered atopic dermatitis lesions.
Restrained inflammatory progression with thinner epidermis and fewer infiltrated mast cells compared with the DNFB model group.
- RT-PCR
- Cytoplasmic-Nuclear Fractionated Protein Extraction
- RNA extraction experimental
- Pull-down
- Immunoprecipitation
- ROS/oxidative-stress fluorescent staining
- TPA/Croton Oil Ear Edema and Dermatitis
- Protocol for Bimolecular Fluorescence Complementation (BiFC) Assay
- Real Time qPCR (Q-PCR)
- Co-Immunoprecipitation
- Protocol for Yeast Two-Hybrid (Y2H) Assay
Chemical Information
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Molecular Weight 1212.06
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Formula C50H38F10IrN8O3P
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SMILES
CC1=C(C2=CC=CC=[C-]2[Ir+3]345([N]6=C(N(CCCNC(CC(C(O)=O)=C)=O)C7=C6C=CC=C7)C8=[N]5C=CC=C8)[C-]9=CC=CC=C9C%10=[N]4C(C=C(F)C(F)=C%11)=C%11N=C%10C)[N]3=C(C=C(F)C(F)=C%12)C%12=N1.F[P-](F)(F)(F)(F)F
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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 PPI-IN-2 Related Classifications
HY-189433 Related Classifications
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