BAY 11-7082 - NF-κB and NLRP3 Inhibitor

InvitroFit™ Inflammasome inhibitor

ABOUT

NF-κB inhibitor - NLRP3 inhibitor

BAY 11-7082 was first described as an irreversible inhibitor of the NF-κB pathway [1]. A number of reports have since shown that BAY 11-7082 has multiple targets, including the NLRP3 (NOD-like receptor pyrin domain-containing protein 3, cryopyrin, or NALP3) inflammasome sensor [2]. The multiprotein NLRP3 inflammasome complex is a key player in innate immunity.

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Modes of action:

Inhibition of NF-κB translocation into the nucleus:BAY11-7082 inhibits the phosphorylation of IκB-α, which is essential for the release of NF-κB from the cytosolic IκB-α/ NF-κB complex [1]. The transcription factor NF-κB regulates multiple aspects of innate and adaptive immune functions and serves as a pivotal mediator of inflammatory responses.

Inhibition of inflammasome responses: BAY 11-7082 may inhibit the inflammasome responses indirectly by preventing the nuclear translocation of NF-κB at the priming step. Moreover, BAY 11-7082 has been shown to exhibit direct inhibitory functions on the NLRP3 inflammasome by blocking the sensor's ATPase activity [2].
 

Key features:

  • Potent inhibitor of NF-κB and the NLRP3 inflammasome
  • Does not inhibit the NLRP1 inflammasome
  • InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested

 

More details Read our review on the NLRP3 inflammasome.

 

References

1. Pierce JW. et al., 1997. Novel Inhibitors of Cytokine-induced Ikappa Balpha Phosphorylation and Endothelial Cell Adhesion Molecule Expression Show Anti-inflammatory Effects in Vivo.J. Biol. Chem., 272: 21096.
2. Juliana C. et al, 2010. Anti-inflammatory Compounds Parthenolide and Bay11-7082 Are Direct Inhibitors of the Inflammasome. J. Biol Chem. 285(13): 9792–9802. 

All products are for research use only, and not for human or veterinary use.

InvitroFit™

InvitroFit™ is a high-quality standard specifically adapted for in vitro studies of inhibitors. InvitroFit™ products are highly pure (≥95%) and guaranteed free of bacterial contamination, as confirmed using HEK Blue™ TLR2 and HEK Blue™ TLR4 cellular assays. Each lot is rigorously tested for functional activity using validated (or proprietary) cellular models. This grade ensures reliability and reproducibility for your research applications.

SPECIFICATIONS

Specifications

CAS number
19542-67-7
Chemical formula

C10H9NO2S

Molecular weight
207.25 g/mol
Purity
≥ 95% (UHPLC)
Solubility

25 mg/ml in DMSO, 15 mg/ml in ethanol

Working concentration

1-10 μM for cell culture assays

Endotoxin

Negative (tested using EndotoxDetect™ assay)

Tested applications

In vitro Inflammasome cellular assays

Quality control

Each lot is functionally tested and validated using cellular assays.

CONTENTS

Contents

  • Product: 
    BAY 11-7082
  • Cat code: 
    tlrl-b82
  • Quantity: 
    10 mg

Shipping & Storage

  • Shipping method:  Room temperature
  • Storage:

    • -20°C
    Stability: The reconstituted product is stable for at least 3 months at -20 °C.

    Caution:

    • Avoid repeated freeze-thaw cycles

Details

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 Bay 11-7082:

Chemical structure of Bay 11-7082

DOCUMENTS

Documents

BAY 11-7082

Technical Data Sheet

Safety Data Sheet

Validation Data Sheet

Certificate of analysis

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