Uses
In the classical pathway of NF-κB activation, phosphorylation of the inhibitor of NF-κB (IκBα) releases the inhibitor from NF-κB, allowing IκBα degradation and NF-κB activation and nuclear import. BAY-11-7085 is an irreversible inhibitor of IκBα phosphorylation, preventing activation of NF-κB by cytokines and lipopolysaccharide (IC50 = 10 μM). It blocks gene expression that is regulated through the classical pathway of NF-κB activation and in this way blocks apoptosis, cell adhesion, and inflammation. BAY-11-7085 is also used to study IκBα actions that are independent of NF-κB signaling.
Uses
Bay 11-7085 has been used as:
- nuclear factor-κB inhibitor in Panc-1 cells, macrophages
- inhibitory κB kinase IKK inhibitor in human astrocytoma cells U87MGs
- phospho-p65 inhibitor human monocyte cell line THP-1
Definition
ChEBI: BAY11-7085 is a sulfone that is benzene substituted by [(E)-2-cyanoethenyl]sulfonyl and tert-butyl groups at position 1 and 4, respectively. It is an irreversible inhibitor of IkappaB-alpha phosphorylation in cells (IC50 = 10 muM) and prevents the activation of NF-kappaB. It has a role as an anti-inflammatory agent, a ferroptosis inducer, a NF-kappaB inhibitor, an apoptosis inducer, an autophagy inducer, an antibacterial agent, an EC 2.7.11.10 (IkappaB kinase) inhibitor and an antineoplastic agent. It is a nitrile, a sulfone and a member of benzenes.
Biological Activity
Irreversible inhibitor of TNF- α -stimulated I κ B α phosphorylation (IC 50 ~ 10 μ M); leads to decreased NF- κ B and subsequent decreased expression of adhesion molecules. Also reversibly activates MAP kinases and stimulates apoptosis. Anti-inflammatory in vivo .
Biochem/physiol Actions
Bay 11-7085 inactivates peroxisome proliferator-activated receptors γ (PPAR-γ) and increases the microtubule-associated proteins 1A/1B light chain 3B (LC3B), a marker of autophagy resulting in apoptosis in human synovial fibroblasts. It promotes apoptosis in pancreatic carcinoma and may serve as radiotherapy-sensitizing drug. BAY 11-7085 decreases B-cell lymphoma 2 (Bcl-2) by inhibiting pI-κBα (inhibitor of nuclear factor κ B kinase subunit α
References
[1]nasu k1, nishida m, ueda t, yuge a, takai n, narahara h. application of the nuclear factor-kappab inhibitor bay 11-7085 for the treatment of endometriosis: an in vitro study. am j physiol endocrinol metab. 2007 jul;293(1):e16-23
