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BAY 11-7082

Cat. No. M2040
BAY 11-7082 Structure
Synonym:

BAY 11-7821

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 58  USD58 In stock
5mg USD 50  USD50 In stock
10mg USD 63  USD63 In stock
25mg USD 110  USD110 In stock
50mg USD 202  USD202 In stock
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Quality Control & Documentation
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
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 Km factor for a mouse and then divide by the Km 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.

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Keywords: BAY 11-7082, BAY 11-7821 supplier, IκB/IKK, inhibitors, activators

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