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NF-κB and NLRP3 inflammasome inhibitor

Isoliquiritigenin Unit size Cat. code Docs Qty Price
IκB-α inhibitor - NLRP3 inflammasome inhibitor
10 mg
inh-ilg
+-
$145.00

NF-κB inhibitor - NLRP3 inhibitor

Inhibitory activity of Isoliquiritigenin
Inhibitory activity of Isoliquiritigenin

Isoliquiritigenin has multiple effects on the immune system. It exhibits antioxidant, anti-inflammatory, and anti-tumor activities [1]. Its targets include NF-κB and the NLRP3 inflammasome.

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.  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.

MODE OF ACTION OF ISOLIQUIRITIGENIN:

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 [2]. Another report suggests it may exhibit inhibitory action on NLRP3-induced ASC oligomerization [3]. 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 [3].

KEY FEATURES OF ISOLIQUIRITIGENIN:

  • Potent inhibitor of the NLRP3 inflammasome
  • Each lot is highly pure (≥98%) and functionally tested

 

Read our review on the NLRP3 inflammasome.

 

References:

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.

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Specifications

Solubility: 10 mg/ml in DMSO and 25 mg/ml in ethanol

CAS number: 961-29-5

Formula: C15H12O4

Molecular weight: 256 g/mol

Quality control:

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Contents

  • 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.

Alert Avoid repeated freeze-thaw cycles.

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Details

Chemical structure of Isoliquiritigenin: 

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