1. NF-κB Apoptosis
  2. NF-κB Apoptosis
  3. NF-κB-IN-4

NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research.

For research use only. We do not sell to patients.

NF-κB-IN-4 Chemical Structure

NF-κB-IN-4 Chemical Structure

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 192 In-stock
Solution
10 mM * 1 mL in DMSO USD 192 In-stock
Solid
5 mg USD 175 In-stock
10 mg USD 280 In-stock
25 mg USD 560 In-stock
50 mg USD 900 In-stock
100 mg USD 1450 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research[1].

In Vitro

NF-κB-IN-4 (compound 17) (0-10 μM, 24 h) shows high anti-inflammatory activity[1].
NF-κB-IN-4 (0-5 μM, 24 h) significantly decreases the LPS-induced p-IκBα expression levels, significantly inhibits the phosphorylation of IκBα and the expression of three proteins (NLRP3, ASC and caspase-1) in BV2 cells[1].
NF-κB-IN-4 (0-5 μM, 24 h) induces LPS-induced apoptosis in BV2 cells in a dose-dependent manner[1].

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

Cell Cytotoxicity Assay

Cell Line: BV2 microglia cells[1]
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 h
Result: Showed high anti-inflammatory activity, with the survival rate of BV2 microglia cells of 97.4%, inhibition rates against TNF-α and IL-6 release of 60.8% and 80.2%, respectively.

Western Blot Analysis

Cell Line: BV2 cells[1]
Concentration: 0, 1.25, 2.5, 5 μM
Incubation Time: 24 h
Result: Significantly decreased the LPS-induced p-IκBα expression levels, significantly inhibited the phosphorylation of IκBα and the expression of three proteins (NLRP3, ASC and caspase-1) in BV2 cells.

Apoptosis Analysis

Cell Line: BV2 cells[1]
Concentration: 0, 2.5, 5 μM
Incubation Time: 24 h
Result: Induced LPS-induced apoptosis in BV2 cells in a dose-dependent manner, with the apoptosis rates of 30.7% (2.5 μM) and 13.0% (5 μM), respectively.
Molecular Weight

322.34

Formula

C18H15FN4O

Appearance

Solid

Color

Off-white to light yellow

SMILES

COC1=CC(C2=C3CCC4=C(C3=NC(N)=N2)C=C(C=C4)F)=CN=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (310.23 mM; ultrasonic and warming and heat to 150°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1023 mL 15.5116 mL 31.0231 mL
5 mM 0.6205 mL 3.1023 mL 6.2046 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1023 mL 15.5116 mL 31.0231 mL 77.5579 mL
5 mM 0.6205 mL 3.1023 mL 6.2046 mL 15.5116 mL
10 mM 0.3102 mL 1.5512 mL 3.1023 mL 7.7558 mL
15 mM 0.2068 mL 1.0341 mL 2.0682 mL 5.1705 mL
20 mM 0.1551 mL 0.7756 mL 1.5512 mL 3.8779 mL
25 mM 0.1241 mL 0.6205 mL 1.2409 mL 3.1023 mL
30 mM 0.1034 mL 0.5171 mL 1.0341 mL 2.5853 mL
40 mM 0.0776 mL 0.3878 mL 0.7756 mL 1.9389 mL
50 mM 0.0620 mL 0.3102 mL 0.6205 mL 1.5512 mL
60 mM 0.0517 mL 0.2585 mL 0.5171 mL 1.2926 mL
80 mM 0.0388 mL 0.1939 mL 0.3878 mL 0.9695 mL
100 mM 0.0310 mL 0.1551 mL 0.3102 mL 0.7756 mL
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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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Product Name:
NF-κB-IN-4
Cat. No.:
HY-144765
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