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.
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Regulatory Status |
RUO – Research Use Only |
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