NSC 319726 (ZMC1)

Catalog No.S7149 Batch:S714901

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Technical Data

Formula

C11H14N4S
Molecular Weight 234.32 CAS No. 71555-25-4
Solubility (25°C)* In vitro DMSO 19 mg/mL (81.08 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description NSC 319726 (ZMC1) 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.
Targets
p53 (R175) [1]
8 nM
In vitro 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. [1]
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. [1]
Features An allele-specific p53 mutant reactivator.

Protocol (from reference)

Kinase Assay:[1]
  • 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.
Cell Assay:[1]
  • Cell lines

    MEF with p53 mutations

  • Concentrations

    ~10 μM

  • Incubation Time

    3 days

  • Method

    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.
Animal Study:[1]
  • Animal Models

    p53+/+, p53-/- and p53R172H knockin mice

  • Dosages

    5-10 mg/kg/day, up to 7 days

  • Administration

    i.p.

Selleck's NSC 319726 (ZMC1) has been cited by 6 publications

Assessment of the In Vitro and In Vivo Antifungal Activity of NSC319726 against Candida auris [ Microbiol Spectr, 2021, 9(3):e0139521] PubMed: 34730380
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
The Global Phosphorylation Landscape of SARS-CoV-2 Infection [ Cell, 2020, 182(3):685-712.e19] PubMed: 32645325
Arsenic Trioxide Rescues Structural p53 Mutations through a Cryptic Allosteric Site [ Cancer Cell, 2020, S1535-6108(20)30605-X] PubMed: 33357454
Copper-Binding Small Molecule Induces Oxidative Stress and Cell-Cycle Arrest in Glioblastoma-Patient-Derived Cells. [ Cell Chem Biol, 2018, 25(5):585-594] PubMed: 29576531
Small-Molecule Reactivation of Mutant p53 to Wild-Type-like p53 through the p53-Hsp40 Regulatory Axis [ Chem Biol, 2015, 22(9):1206-16] PubMed: 26320861

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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