1. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  2. NF-κB Heme Oxygenase (HO) Interleukin Related Reactive Oxygen Species (ROS) NO Synthase
  3. 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.

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Nrf2 activator-24

Nrf2 activator-24 Chemical Structure

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Description

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[1].

In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: HaCaT human keratinocytes
Concentration: up to 1 μM
Incubation Time: 24 h
Result: Showed no cytotoxic effects on HaCaT keratinocytes at concentrations up to 1 μM.

Western Blot Analysis[1]

Cell Line: HaCaT human keratinocytes
Concentration: 0.003, 0.01, 0.03, 0.1 μM
Incubation Time: 3 h
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.

Western Blot Analysis[1]

Cell Line: HaCaT human keratinocytes
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 6 h (Nrf2); 12 h (HO-1, GCLM)
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).

Western Blot Analysis[1]

Cell Line: TNF-α+IFN-γ-stimulated HaCaT human keratinocytes
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 3 h pretreatment; 24 h cytokine stimulation
Result: Suppressed TNF-α+IFN-γ-induced IL-1β protein expression in a concentration-dependent manner.

Western Blot Analysis[1]

Cell Line: LPS-stimulated Raw264.7 mouse macrophages
Concentration: 0.03, 0.1, 0.3, 1 μM
Incubation Time: 3 h pretreatment; 24 h LPS stimulation
Result: Suppressed LPS-induced iNOS protein expression in a concentration-dependent manner.
In Vivo

Nrf2 activator-24 (0.1-0.5%; topical administration; once every 2 days; days 8-14) effectively alleviates DNCB-induced atopic dermatitis-like symptoms in BALB/c mice[1].

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

Animal Model: BALB/c (6-week-old male, DNCB-induced atopic dermatitis model)[1]
Dosage: 0.1%; 0.5%
Administration: topical; every other day; Days 8-14, 1 hour after DNCB challenge
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.
Molecular Weight

360.09

Formula

C14H10Cl2O2Se

SMILES

ClC1=C([Se](/C=C/C2=CC=CC=C2Cl)(=O)=O)C=CC=C1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Nrf2 activator-24
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HY-182040
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