NSC-319726 (ZMC1), a mutant p53R175 reactivator, suppresses growth of fibroblasts that expresses the p53R175 mutation (IC50 = 8 nM).

p53 (R175):8 nM

在p53(R172H/R172H)小鼠中, NSC319726（5 mg/kg）会产生较强的毒性,存活率低.在TOV112D-p53(R175H) 移植瘤中,NSC319726能够抑制瘤细胞生长.

在突变型p53的细胞中,NSC319726（IC50=8 nM）可使突变蛋白发生WT样构象变化,从而修复序列特异性的p53转录。

MTS: 5,000 cells of TOV112D cells (5,000 cells/well, in 100 ml culture) are cultured in 96-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compounds. The growth is measured by MTS reagent and Victor Plate reader instrument after incubation for 3 days.

Viability assays are done. The cells (5×104 cells/well, in 1 ml culture) are cultured in a 12-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compound. The growth is measured by Guava ViaCount reagent and Guava PCA instrument after incubation for 3 days.(Only for Reference)