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.
|Source||Biochem J (2013). Figure 2. Bay 11-7082|
|Cell Lines||human IL-1R cells|
|Incubation Time||1 h|
|Results||BAY 11-7082 completely suppressed the LPS-stimulated and IL-1-stimulated phosphorylation of the activation loop of IKKβ.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO >20 mg/mL|
The role of Rac1 in the regulation of NF-κB activity, cell proliferation, and cell migration in non-small cell lung carcinoma.
Gastonguay A, et al. Cancer Biol Ther. 2012 Jun;13(8):647-56. PMID: 22549160.
The inhibitor of I kappa B alpha phosphorylation BAY 11-7082 prevents NMDA neurotoxicity in mouse hippocampal slices.
Goffi F, et al. Neurosci Lett. 2005 Apr 4;377(3):147-51. PMID: 15755516.
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.
Mori N, et al. Blood. 2002 Sep 1;100(5):1828-34. PMID: 12176906.
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