NSC 319726 (ZMC1)

製品コードS7149 バッチS714901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H14N4S
分子量 234.32 CAS No. 71555-25-4
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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]
特徴 An allele-specific p53 mutant reactivator.

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 MEF with p53 mutations
濃度 ~10 μM
反応時間 3 days
実験の流れ 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.
動物実験 動物モデル p53+/+, p53-/- and p53R172H knockin mice
投薬量 5-10 mg/kg/day, up to 7 days
投与方法 i.p.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。