产品说明书
NSC319726
 |
同义名 : | ZMC1 |
| CAS号 : | 71555-25-4 | |
| 货号 : | A213189 | |
| 分子式 : | C11H14N4S | |
| 纯度 : | 99%+ | |
| 分子量 : | 234.321 | |
| MDL号 : | MFCD01665446 | |
| 存储条件： |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 30 mg/mL(128.03 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | NSC319726 is a p53R175 mutant reactivator, which can restores WT structure and function to the p53R175 mutant. Cell lines with p53R175 mutant, including MEF cell lines from p53R172H/R172H mice, HOP92 (R175L), TOV112D (R175H), AU565 (R175H), SK-BR-3 (R175H), exhibited more sensitivity to cell lines with p53 WT, p53R248, or p53R273. NSC319726 could induce a ‘‘WT-like’’ conformational change in the p53-175 mutant protein and reactivate its function as p53 WT, as treatment with 1μM NSC319726 led a significant decrease of p53 protein level in TOV112D cells (R175 mutant) within 8h and restored p53 protein level to normal level at 12h later, which can be eliminated by Mdm2 antagonist Nutlin-3. Administration of NSC319726 at dose of 5 or 10mg/kg, i.p., for 7 days, selectively killed p53R172H knockin mice with extensive apoptosis. Daily intravenous administration of NSC319726 at 1 or 0.1mg/kg selectively inhibited xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner. | ||
| 作用机制 | NSC319726 induced a ‘‘WT-like’’ conformational change in the p53-175 mutant protein. This activity depends upon the zinc ion chelating properties of the compound as well as redox changes.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
4.27mL 0.85mL 0.43mL |
21.34mL 4.27mL 2.13mL |
42.68mL 8.54mL 4.27mL |
| 参考文献 |
|---|