BAY 11-7082

Biological Activity

BAY 11-7082 (BAY 11-7821) is an irreversible inhibitor of TNF-α-stimulated IκBα phosphorylation. BAY 11-7082 selectively and irreversibly inhibits NF-κB activation by blocking TNF-α-induced phosphorylation of IκB-α without affecting constitutive IκB-α phosphorylation. BAY 11-7082 inhibits the TNF-α-induced surface expression of adhesion molecules ICAM-1, VCAM-1, and E-selectin in human endothelial cells with IC50 values of 5-10 µM. BAY 11-7082 also reversibly activates MAP kinases and stimulates apoptosis. BAY 11-7082 rapidly and efficiently reduced the DNA binding of NF-kappaB in HTLV-I-infected T-cell lines and down-regulated the expression of the antiapoptotic gene, Bcl-x(L), regulated by NF-kappaB, whereas it had little effect on the DNA binding of another transcription factor, AP-1. 

Furthermore, BAY 11-7082- induced apoptosis of primary ATL cells was more prominent than that of normal peripheral blood mononuclear cells, and apoptosis of these cells was also associated with down-regulation of NF-kappaB activity.

Product Citations

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  Foods. 2022 Jan 12;11(2):196.

  Impact of the Plastein Reaction of Casein Hydrolysates in the Presence of Exogenous Amino Acids on Their Anti-Inflammatory Effect in the Lipopolysaccharide-Stimulated Macrophages
  BAY 11-7082 purchased from AbMole

• 

  J Inflamm Res. 2021 Mar 17;14:917-928.

  Stable Cells with NF-KB-ZsGreen Fused Genes Created by TALEN Editing and Homology Directed Repair for Screening Anti-inflammation Drugs.
  BAY 11-7082 purchased from AbMole

• 

  J Inflamm Res. 2021 Mar 17;14:917-928.

  Stable Cells with NF-κB-ZsGreen Fused Genes Created by TALEN Editing and Homology Directed Repair for Screening Anti-inflammation Drugs
  BAY 11-7082 purchased from AbMole

• 

  Mediators Inflamm. 2019 Feb 19;2019:1082497.

  Astragaloside IV Suppresses High Glucose-Induced NLRP3 Inflammasome Activation by Inhibiting TLR4/NF-κB and CaSR.
  BAY 11-7082 purchased from AbMole

Customer Product Validations & Biological Datas

	Source	Biochem J (2013). Figure 2. Bay 11-7082
	Method	immunoblotting
	Cell Lines	human IL-1R cells
	Concentrations	15 μM
	Incubation Time	1 h
	Results	BAY 11-7082 completely suppressed the LPS-stimulated and IL-1-stimulated phosphorylation of the activation loop of IKKβ.

Chemical Information

Molecular Weight	207.25
Formula	C10H9NO2S
CAS Number	19542-67-7
Solubility (25°C)	DMSO 31 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gastonguay A, et al. Cancer Biol Ther. The role of Rac1 in the regulation of NF-κB activity, cell proliferation, and cell migration in non-small cell lung carcinoma.

[2] Goffi F, et al. Neurosci Lett. The inhibitor of I kappa B alpha phosphorylation BAY 11-7082 prevents NMDA neurotoxicity in mouse hippocampal slices.

[3] Mori N, et al. Blood. Bay 11-7082 inhibits transcription factor NF-kappaB and induces apoptosis of HTLV-I-infected T-cell lines and primary adult T-cell leukemia cells.