Nrf2 activator-24
Nrf2 activator-24 is a Nrf2 activator with anti-inflammatory and antioxidant activities. Nrf2 activator-24 promotes the nuclear translocation of Nrf2, thereby inducing the expression of downstream antioxidant and cytoprotective genes. Nrf2 activator-24 inhibits cytokine-driven inflammatory responses in keratinocytes. Nrf2 activator-24 attenuates inflammation, nitrosation and oxidative stress responses in macrophages. Nrf2 activator-24 alleviates local inflammation and atopic dermatitis-like symptoms in DNCB-induced mouse models. Nrf2 activator-24 can be used in research related to atopic dermatitis.
For research use only. We do not sell to patients.
- Formula: C14H10Cl2O2Se
- Molecular Weight:360.09
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Nrf2 activator-24 (various concentrations; 6 h) potently induces Nrf2 nuclear translocation in engineered U2OS cells with an EC50 of 4.9 ± 0.3 nM[1].
Nrf2 activator-24 (up to 1 μM; 24 h) is non-cytotoxic to HaCaT human keratinocytes[1].
Nrf2 activator-24 (0.1 μM; up to 24 h) induces peak Nrf2 nuclear translocation in HaCaT human keratinocytes at 3 h post-treatment, with levels decreasing thereafter up to 24 h[1].
Nrf2 activator-24 (increasing concentrations; 6 h (Nrf2), 12 h (HO-1, GCLM)) induces concentration-dependent increases in Nrf2, HO-1, and GCLM protein expression in HaCaT human keratinocytes, with maximal effects at 1 μM[1].
Nrf2 activator-24 (increasing concentrations; 6 h) induces concentration-dependent increases in HMOX1, GCLM, GCLC, and NQO1 mRNA expression in HaCaT human keratinocytes, with maximal effects at 1 μM[1].
Nrf2 activator-24 (0.03-1 μM; 3 h pretreatment, 24 h cytokine stimulation) concentration-dependently suppresses IL-1β protein expression in TNF-α+IFN-γ-stimulated HaCaT human keratinocytes[1].
Nrf2 activator-24 (0.03-1 μM; 6 h pretreatment, 3 h cytokine stimulation (IL6, TNF); 24 h cotreatment (CCL17, CCL22)) concentration-dependently suppresses IL6, TNF, CCL17, and CCL22 mRNA expression in TNF-α+IFN-γ-stimulated HaCaT human keratinocytes[1].
Nrf2 activator-24 (0.03-1 μM; 3 h pretreatment, 24 h LPS stimulation) concentration-dependently suppresses iNOS protein expression in LPS-stimulated Raw264.7 mouse macrophages[1].
Nrf2 activator-24 (0.03-1 μM; 3 h pretreatment, 24 h LPS stimulation) concentration-dependently suppresses NO production in LPS-stimulated Raw264.7 mouse macrophages[1].
Nrf2 activator-24 (0.1 μM; 9 h pretreatment) effectively reduces H2O2-induced intracellular ROS levels in Raw264.7 mouse macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HaCaT human keratinocytes
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Concentration:up to 1 μM
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Incubation Time:24 h
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Result:Showed no cytotoxic effects on HaCaT keratinocytes at concentrations up to 1 μM.
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Cell Line:HaCaT human keratinocytes
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Concentration:0.003, 0.01, 0.03, 0.1 μM
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Incubation Time:3 h
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Result:Increased nuclear Nrf2 in a concentration-dependent manner.
Induced a significant 3.60 ± 0.11-fold increase in nuclear Nrf2 at 0.003 μM.
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Cell Line:HaCaT human keratinocytes
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Concentration:0.03, 0.1, 0.3, 1 μM
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Incubation Time:6 h (Nrf2); 12 h (HO-1, GCLM)
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Result:Increased Nrf2 protein accumulation to 5.71 ± 0.10-fold at 1 μM (6 h treatment).
Upregulated HO-1 and GCLM expression by 10.58 ± 0.74-fold and 3.44 ± 0.11-fold, respectively, at 1 μM (12 h treatment).
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Cell Line:TNF-α+IFN-γ-stimulated HaCaT human keratinocytes
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Concentration:0.03, 0.1, 0.3, 1 μM
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Incubation Time:3 h pretreatment; 24 h cytokine stimulation
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Result:Suppressed TNF-α+IFN-γ-induced IL-1β protein expression in a concentration-dependent manner.
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Cell Line:LPS-stimulated Raw264.7 mouse macrophages
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Concentration:0.03, 0.1, 0.3, 1 μM
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Incubation Time:3 h pretreatment; 24 h LPS stimulation
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Result:Suppressed LPS-induced iNOS protein expression in a concentration-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (6-week-old male, DNCB-induced atopic dermatitis model)[1]
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Dosage:0.1%; 0.5%
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Administration:topical; every other day; Days 8-14, 1 hour after DNCB challenge
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Result:Significantly reduced dermatitis scores.
Significantly suppressed scratching behavior.
Reduced spleen and lymph node weights in a concentration-dependent manner.
Significantly lowered plasma IgE levels.
Significantly attenuated epidermal thickening.
Significantly reduced eosinophil infiltration in dorsal skin.
Significantly reduced mast cell infiltration in dorsal skin (0.5% group); showed near-significant reduction (0.1% group).
Significantly reduced skin IL-6 protein levels in a concentration-dependent manner.
Significantly restored skin loricrin protein levels.
Chemical Information
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Molecular Weight 360.09
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Formula C14H10Cl2O2Se
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SMILES
ClC1=C([Se](/C=C/C2=CC=CC=C2Cl)(=O)=O)C=CC=C1
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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)
Nrf2 activator-24 Related Classifications
HY-182040 Related Classifications
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