Molecular Weight(MW): 234.32
NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.
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2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.|
|Features||An allele-specific p53 mutant reactivator.|
NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells, shows 10- to 100-fold selectivity over the other hotspot p53 mutants. NSC319276 induces p53(R175)-mutant-dependent apoptosis. NSC319726 treatment induces a WT-like conformational change in the p53(R175) mutant protein that restores sequence-specific p53 transcription. The activity of NSC319726 depends on the zinc ion chelating properties of the compound as well as redox changes. 
|In vivo||NSC319726 (5mg/kg, 7days) exhibits greater toxicity for p53(R172H/R172H) mice, with only 30% survival, as compared to 100% survival for p53+/+ and p53-/- mice. NSC319726 inhibits the growth of TOV112D-p53(R175H) xenografts, but not H460 (p53+/+) and MDAMB468-p53(R273W) xenografts. |
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.
|In vitro||DMSO||19 mg/mL (81.08 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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