NF-κB and NLRP3 inflammasome inhibitor - BAY 11-7082
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IκB-α inhibitor - NLRP3 inflammasome inhibitor
NF-κB inhibitor - NLRP3 inhibitor
BAY 11-7082 was first described as an irreversible inhibitor of the NF-κB pathway . A number of reports have since shown that BAY 11-7082 has multiple targets, including the NLRP3 inflammasome sensor . BAY11-7082 has been reported to display broad-spectrum anti-inflammatory activities and influence various physiological processes [3, 4].
MODES OF ACTION OF BAY 11-7082:
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 . 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: The formation of functional inflammasomes occurs according to a consensual two-step model. The priming step (step 1) induces the NF-κB-dependent transcription of pro-IL-1β and of NLRP3 sensor. The activation step (step 2) triggers the multimerization of the activated sensor with ASC and pro-caspase-1 molecules. This assembly allows caspase-1 self-activation, which in turn induces the maturation and secretion of IL-1β and IL-18 cytokines, along with alarmins, and a pyroptotic cell death driven by the formation of Gasdermin D (GSDMD) lytic pores at the cell membrane. Thus, 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 was shown to exhibit direct inhibitory functions on the NLRP3 inflammasome by blocking the sensor's ATPase activity .
KEY FEATURES OF BAY 11-7082:
- Potent inhibitor of NF-κB and the NLRP3 inflammasome
- Does not inhibit the NLRP1 inflammasome
- Each lot is highly pure (≥95%) and functionally tested
Read our review on inflammasomes.
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.
3. Lee J et al., 2012. BAY 11-7082 Is a Broad-Spectrum Inhibitor with Anti-Inflammatory Activity against Multiple Targets. Med. Inflammation. 2012:416036.
4. Xu C. et al., 2019. Bay 11-7082 facilitates wound healing by antagonizing mechanical injury and TNF-α-induced expression of MMPs in posterior cruciate ligament. Connect. Tissue Res. 60 311.
Bay11-7082 inhibits the NLRP3 inflammasome response in a dose-dependent manner.
THP1-Null2 cells were primed with LPS-EK (1 μg/ml) for 3 h and then stimulated with MSU (150 µg/ml) and increasing concentrations of Bay11-7082. 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.
Working concentration: 1-10 μM
CAS number: 19542-67-7
Molecular weight: 207.25 g/mol
Solubility: 25 mg/ml in DMSO and 15 mg/ml in ethanol
- Purity: ≥95% (UHPLC)
- The inhibitory activity of the product has been validated using cellular assays.
- The absence of bacterial contamination (e.g. lipoproteins and endotoxins) is confirmed using HEK-Blue™ TLR2 and HEK-Blue™ TLR4 cells.
- 10 mg BAY 11-7082 (provided as a translucent film)
BAY 11-7082 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
Chemical structure of Bay 11-7082:
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