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Beschreibung

A cell-permeable steroidal lactone that displays antitumor, anti-inflammatory, radiosensitizing, and immunosuppressive properties. Potently inhibits angiogenesis both in vitro (IC50 = 12 nM against HUVEC proliferation) and in vivo (80% inhibition at 7 µ,g/kg/day in C57BL/6J mice, s.c.) and NF-kappaB activation (IC50 = 500 nM in TNF-alpha-induced endothelial cells) by targeting the ubiquitin-mediated proteasome pathway. At higher concentrations (~5 µ,M) also affects AP-1 transcription and induces cell death.