196309-76-9

An irreversible inhibitor of cytokine-inducible IκBα phosphorylation (IC50=10 μM). In intact HUVECs it inhibits TNFα-induced phosphorylation and degradation of IκBα without affecting constitutive phosphorylation. Inhibition of IκBα phosphorylation and degradation results in the inactivation of NF-κB and NF-κB-dependent expression of endothelial-leukocyte adhesion molecules, E-selectin, VCAM-1 and ICAM-1. BAY 11-7085 displayed potent anti-inflammatory activity in the rat carrageenan paw edema assay and adjuvant arthritis model.

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.

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.

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 .

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

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[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