SCH 529074
An activator of p53; restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay (Kds = 0.6740 and 0.4313, respectively); stimulates DNA binding activity and prevents Hdm-2 ubiquitination of wild-type p53 in vitro; reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM); reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner
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SCH 529074
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