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Chemical Structure| 19542-67-7 Chemical Structure| 19542-67-7

Structure of BAY 11-7082
CAS No.: 19542-67-7

Chemical Structure| 19542-67-7

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BAY 11-7082 is an inhibitor of IκBα phosphorylation and NF-κB. It selectively and irreversibly inhibits TNF-α-induced phosphorylation of IκB-α, decreases NF-κB activity, and reduces the expression of adhesion molecules. Additionally, BAY 11-7082 inhibits ubiquitin-specific proteases USP7 and USP21 (IC50 = 0.19, 0.96 μM, respectively), gasdermin D (GSDMD) pore formation in liposomes, and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.

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Product Details of BAY 11-7082

CAS No. :19542-67-7
Formula : C10H9NO2S
M.W : 207.25
SMILES Code : N#C/C=C/S(=O)(C1=CC=C(C)C=C1)=O
MDL No. :MFCD00712162
InChI Key :DOEWDSDBFRHVAP-KRXBUXKQSA-N
Pubchem ID :5353431

Safety of BAY 11-7082

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BAY 11-7082

pyroptosis
TLR

Isoform Comparison

Biological Activity

Description
BAY 11-7082 acts as an inhibitor of IκBα phosphorylation and NF-κB. It selectively and irreversibly suppresses TNF-α-induced phosphorylation of IκB-α, leading to reduced NF-κB activity and expression of adhesion molecules. Furthermore, BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 values of 0.19 μM and 0.96 μM, respectively. Additionally, it hampers gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis, as well as IL-1β secretion in both human and mouse cells [1][2][3][4][5].
Target
  • E2 conjugating

In Vitro:

Cell Line
Concentration Treated Time Description References
Murine Hypopharyngeal Primary Cells (MHPC) 10 μM 3 times/day for 5 days BAY 11-7082 effectively suppressed acidic bile-induced NF-κB activation and reduced the cancer-related mRNA phenotype. PMC5909679
MDSCs 2.5μM 12 days BAY 11-7082 significantly inhibited the differentiation of MDSCs to osteoclasts, as shown by the marked decrease in TRAP staining and the absence of F-actin ring formation. PMC4679657

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse C57BL/6J mice Topical application 0.25 μM 3 times for 7 days BAY 11-7082 effectively prevented acidic bile-induced NF-κB activation and its associated oncogenic mRNA and miRNA phenotypes through topical application. PMC5909679
C57BL/6 mice Spinal cord injury model Intraperitoneal injection 20 mg/kg Once daily for 3 days BAY 11-7082 inhibited NLRP3 inflammasome activation, reduced neuronal death, attenuated spinal cord anatomic damage, and promoted motor recovery. Furthermore, BAY 11-7082 directly attenuated the levels of NLRP3 inflammasome and proinflammatory cytokines. Moreover, BAY 11-7082 alleviated microglia/macrophage activation, neutrophils infiltration, and reactive gliosis, as well as mitochondrial dysfunction. PMC5657095

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.83mL

0.96mL

0.48mL

24.13mL

4.83mL

2.41mL

48.25mL

9.65mL

4.83mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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