Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NF-κB-IN-4 (compound 17) is a potent inhibitor of NF-κB pathway which can cross blood brain barrier (BBB). NF-κB-IN-4 shows potential anti-neuroinflammatory activity with low toxicity which can be used for the research of neuroinflammation related diseases. NF-κB-IN-4 can block the IκBα activation and phosphorylation, reduce NLRP3 expression, therefore inhibiting NF-κB activation [1].
Description | NF-κB-IN-4 (compound 17) is a potent inhibitor of NF-κB pathway which can cross blood brain barrier (BBB). NF-κB-IN-4 shows potential anti-neuroinflammatory activity with low toxicity which can be used for the research of neuroinflammation related diseases. NF-κB-IN-4 can block the IκBα activation and phosphorylation, reduce NLRP3 expression, therefore inhibiting NF-κB activation [1]. |
In vitro | NF-κB-IN-4 (compound 17), at concentrations ranging from 0-10 μM over 24 hours, exhibits strong anti-inflammatory effects. Notably, at dosages between 0-5 μM for the same duration, it significantly reduces LPS-induced p-IκBα levels and inhibits IκBα phosphorylation along with the expression of NLRP3, ASC, and caspase-1 proteins in BV2 microglial cells. Furthermore, NF-κB-IN-4 prompts dose-dependent apoptosis in these cells following LPS exposure. In cell cytotoxicity assays using BV2 microglia cells, a high anti-inflammatory action is observed with a 97.4% cell survival rate, and inhibitory effects on TNF-α and IL-6 release by 60.8% and 80.2%, respectively, over a 24-hour period at concentrations of 0, 2.5, 5, and 10 μM. Western blot analyses confirm the significant decrease in LPS-induced p-IκBα expression and inhibition of IκBα phosphorylation and NLRP3, ASC, and caspase-1 protein expression at concentrations of 0, 1.25, 2.5, and 5 μM. Apoptosis analysis further validates the induction of LPS-induced apoptosis in a dose-dependent manner with apoptosis rates of 30.7% at 2.5 μM and 13.0% at 5 μM. |
Molecular Weight | 322.34 |
Formula | C18H15FN4O |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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