NF-κB and NLRP3 inflammasome inhibitor
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IκB-α inhibitor - NLRP3 inflammasome inhibitor
NF-κB inhibitor - NLRP3 inhibitor
Isoliquiritigenin has multiple effects on the immune system. It exhibits antioxidant, anti-inflammatory, and anti-tumor activities . Its targets include NF-κB and the NLRP3 (NOD-like receptor pyrin domain-containing protein 3, cryopyrin, or NALP3) inflammasome sensor. The multiprotein NLRP3 inflammasome complex is a key player in innate immunity.
Mode of action:
Specifically, isoliquiritigenin inhibits TNF-α-induced NF-κB activation and translocation to the nucleus by blocking IκB kinase activity, suggesting that it can block inflammasome priming . Another report suggests it may exhibit inhibitory action on NLRP3-induced ASC oligomerization . In addition, it has been demonstrated that isoliquiritigenin is a more potent NLRP3 inflammasome inhibitor than other inflammasome inhibitors such as parthenolide and glybenclamide. Of note, isoliquiritigenin does not inhibit the AIM2 inflammasome .
- Potent inhibitor of the NLRP3 inflammasome
- Each lot is highly pure (≥98%) and functionally tested
Read our review on the NLRP3 inflammasome.
Download our Practical guide on Inflammasomes.
1. Jung SK. et al., 2014. Isoliquiritigenin induces apoptosis and inhibits xenograft tumor growth of human lung cancer cells by targeting both wildtype and L858R/T790M mutant EGFR. J Biol Chem. 289(52):35839-48.
2. Kumar S. et al., 2007. Isoliquiritigenin inhibits IκB kinase activity and ROS generation to block TNF-α induced expression of cell adhesion molecules on human endothelial cells. Biochem. Pharmacol. 73(10): 1602-12.
3. Honda H. et al., 2014. Isoliquiritigenin is a potent inhibitor of NLRP3 inflammasome activation and diet-induced adipose tissue inflammation. J Leukoc Biol. 96(6):1087-100.
Isoliquiritigenin inhibits the NLRP3 inflammasome response in a dose-dependent manner.
THP1‑Null2 cells, primed with LPS-EK (1 μg/ml for 3 h), were stimulated with MSU (150 µg/ml) and increasing concentrations of isoliquiritigenin. After overnight incubation, IL-1β secretion was analyzed by adding 50 µl of supernatant from treated THP1-Null2 cells to HEK‑Blue™ IL‑1β cells. IL‑1β‑induced activation of NF‑κB was assessed by measuring the levels of SEAP in the supernatant of HEK-Blue™ IL-1β cells using QUANTI‑Blue™ Solution, a SEAP detection reagent, and by reading the optical density (OD) at 655 nm. Data are shown as a percentage (%) inhibition of the maximal response for the ligand with no inhibitor.
Solubility: 10 mg/ml in DMSO and 25 mg/ml in ethanol
CAS number: 961-29-5
Molecular weight: 256 g/mol
- Purity ≥98% (UHPLC)
- The inhibitory activity of the product has been validated in inflammasome cellular assays using THP1-Null2 and HEK-Blue™ IL-1β cells.
- The absence of bacterial contamination (e.g. lipoproteins and endotoxins) has been confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.
- 10 mg Isoliquiritigenin (provided as a powder)
Isoliquiritigenin is shipped at room temperature.
Upon receipt, store at -20°C.
Resuspended product is stable for at least 6 months when properly stored.
Avoid repeated freeze-thaw cycles.Back to the top
The NLRP3 Inflammasome:
The NLRP3 inflammasome is an innate immune sensor that is activated by a two-step process; a first signal (‘priming’) provided mainly by bacterial components or endogenous cytokines involves NF-κB induction, while the second signal provided by a wide array of stimuli including microbial toxins, endogenous molecules or crystalline substances and leads to inflammasome assembly and activation [1, 2]. This triggers inflammasome multimerization and caspase-1 activation with the subsequent cleavage of interleukin-1β (IL-1β)/IL-18 and the pore-forming protein Gasdermin D (GSDMD) into their active forms. Additionally, the activation of the inflammasome also leads to alarmin secretion and pyroptosis, a form of immunogenic cell death.
1. Swanson K.V. et al., 2019. The NLRP3 inflammasome: molecular activation and regulation to therapeutics. Nat. Rev. Immunol. 19:477.
2. Groslambert M. & Py B. 2018. Spotlight on the NLRP3 inflammasome pathway. J. Inflamm. Res. 11:359.
Chemical structure of Isoliquiritigenin:
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