产品描述:
NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA.{36321} It selectively inhibits growth of human tumor cell lines containing mutant p53 over those containing wild-type p53 (IC50s = 0.1-1 and >10 μM, respectively). NSC 319726 induces apoptosis in TOV112D (p53R175H), but not OVCAR3 (p53R248W) or SKOV3 (p53-/-), cells at a concentration of 1 μM. It restores a wild-type conformation to human p53175 and mouse p53R172 mutant proteins and induces expression of p53 target genes in TOV112D cells. In vivo, NSC 319726 (1 mg/kg) inhibits tumor growth in TOV112D, but not H460 (p53+/+), mouse xenograft model. NSC 319726 also has broad-spectrum antifungal activity (MIC50s = 0.1-2 μg/ml against a panel of pathogenic fungi) with >800-fold selectivity for fungi over human HUH-7 and HepG2 cells.{36322}