NSC 319726

NSC 319726 is a reactivator of p53R175, a p53 conformational mutant that cannot bind DNA. 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.Formal Name: 2-[1-(2-pyridinyl)ethylidene]hydrazide, 1-azetidinecarbothioic acid. CAS Number: 71555-25-4. Molecular Formula: C11H14N4S. Formula Weight: 234.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 16 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 14 mg/ml, Ethanol: isnoluble, PBS (pH 7.2): isnoluble. lambdamax: 217, 309 nm. SMILES: C/C(C1=CC=CC=N1)=N\NC(N2CCC2)=S. InChi Code: InChI=1S/C11H14N4S/c1-9(10-5-2-3-6-12-10)13-14-11(16)15-7-4-8-15/h2-3,5-6H,4,7-8H2,1H3,(H,14,16)/b13-9+. InChi Key: XDHBUMNIQRLHGO-UKTHLTGXSA-N.