Product nameNSC 319726, p53(R175) mutant reactivator
DescriptionSelective p53(R175) mutant reactivator
- 1-Azetidinecarbothioic acid [1-(2-pyridinyl)ethylidene]hydrazide
p53(R175) mutant reactivator. Inhibits growth of fibroblasts expressing the p53(R175) mutation (IC50 = 8 nM), shows no inhibition for p53 wild-type cells. Displays 10- to 100-fold selectivity over the other hotspot p53 mutants and induces p53(R175)-mutant-dependent apoptosis. Also inhibits growth of xenograft tumors expressing the p53(R175) mutation in vivo. Restores p53 wild-type structure by functioning as a zinc-metallochaperone.
Storage instructionsStore at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 75 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
This product has been referenced in:
- Bykov VJ & Wiman KG Mutant p53 reactivation by small molecules makes its way to the clinic. FEBS Lett 588:2622-7 (2014). Read more (PubMed: 24768524) »
- Yu X et al. Small molecule restoration of wildtype structure and function of mutant p53 using a novel zinc-metallochaperone based mechanism. Oncotarget 5:8879-92 (2014). Read more (PubMed: 25294809) »
- Yu X et al. Allele-specific p53 mutant reactivation. Cancer Cell 21:614-25 (2012). Read more (PubMed: 22624712) »