White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. 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 µg/kg/day in C57BL/6J mice, s.c.) and NF-kB activation (IC50 = 500 nM in TNF-a-induced endothelial cells) by targeting the ubiquitin-mediated proteasome pathway. At higher concentrations (~5 µM) also affects AP-1 transcription and induces cell death. Purity: ≥94% by HPLC. RTECS KE7288500, CAS 5119-48-2. Ref.: Mohan, R., et al. 2004. Angiogenesis 7, 115. Jeyaprakasam, B., et al. 2003. Life Sci. 74, 125. Devi, P.U., et al. 1995. Cancer Lett. 95, 189. Kupchan, S.M., et al. 1969. J. Org. Chem. 34, 3858. |