Mouse double minute 2 protein (Mdm2) is an E3 ubiquitin-protein ligase that binds and ubiquitinates the tumor suppressor p53, leading to its degradation by the proteasome.{11628} SP 141 is a cell-permeable inhibitor of Mdm2 (Ki = 28 nM).{27642} Binding of Mdm2 by SP 141 promotes its auto-ubiquitination and proteasomal degradation.{27642,29204} SP 141 induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines and inhibits xenograft tumor growth in vivo.{27642,29204} This compound has a short half-life in plasma and wide tissue distribution in tumor-bearing nude mice.{29203}
产品描述
A cell-permeable inhibitor of Mdm2 (Ki = 28 nM); promotes Mdm2 auto-ubiquitination and proteasomal degradation; induces cell cycle arrest and apoptosis in breast and pancreatic cancer cell lines and inhibits xenograft tumor growth in vivo
