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BMS-345541 is a highly selective, cell-permeable, small molecule inhibitor of IκB kinase (IKK), specifically targeting IKK-2 (IC50 = 0.3 μM) and, to a lesser extent, IKK-1 (IC50 = 4 μM). It functions by binding an allosteric site on IKK, blocking the phosphorylation of IκBα, thereby inhibiting NF-κB-dependent transcription. Through this mechanism, BMS-345541 suppresses the production of downstream inflammatory cytokines (such as TNF-α, IL-1β, IL-6, and IL-8), induces apoptosis in cancer cells, and reduces tumorigenicity in preclinical models. It has shown efficacy in murine models of melanoma, breast cancer, and collagen-induced arthritis, with significant anti-inflammatory and anticancer activity. BMS-345541 is not approved for human or clinical use and is primarily utilized as a research tool compound for studying NF-κB/IKK signaling and disease models related to inflammation and cancer[1][5][7][9].
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