Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling.{25314} It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53.{25314} CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65.{25314} It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 µM).{25314} CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.{25314}
产品描述
A dual modulator of p53-MDM2 interaction and NF-κB signaling; binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53; inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65; inhibits cancer cell growth in vitro and in vivo
