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CAS No.: 803647-40-7

NSC59984 Catalog No. CSN17369

Synonyms: NSC 59984

NSC 59984 is a reactivator of p53 which targets various mutant p53 to restore wild-type p53 pathway via the activation of p73 in cancer cells. It could induce p53 mutant protein degradation via MDM2-mediated ubiquitination.

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实验方案

技术信息

生物活性

描述NSC59984 is a mutant p53 reactivator, which can both restore wild-type p53 signaling through stimulation of transcription factor p73 and deplete mutant p53 GOF. NSC59984 at 25μM selectively restored p53-responsive transcriptional activity in mutant p53-expressing tumor cells, SW480 (mutant p53 R273H, P309S) and DLD-1 (mutant p53 S241F) cells, as endogenous protein levels of p21, Puma, Noxa, and DR5, target genes of p53, were significantly upregulated. NSC59984 induced cell death in tumor cells with EC50 values ranging in 8.38-110.49μM but not normal cells with little or no genotoxicity. NSC59984 induced mutant p53 protein degradation via MDM2 and the ubiquitin–proteasome pathway. NSC59984 treatment downregulated various mutant p53 proteins in a dose-dependent manner in SW480, DLD-1, Hop92 (mutant p53 R175L), and RXF393 cells (mutant p53 R175H). In contrast, wild-type p53 protein was upregulated in MRC-5 normal cells and HCT116 cancer cells treated with 50μM of NSC59984. Administration of NSC59984 at dose of 45mg/kg, i.p., significantly repressed DLD-1 xenograft tumor growth.
作用机制NSC59984 restores wild-type p53 signaling via p73 activation in mutant p53-expressing colorectal cancer cells.^[1]
动物研究
剂量
Mice: 45 mg/kg^[1] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 45 mg/kg^[1] (i.p.)
给药途径	i.p.

[1] Zhang S, Zhou L, et al. Small-Molecule NSC59984 Restores p53 Pathway Signaling and Antitumor Effects against Colorectal Cancer via p73 Activation and Degradation of Mutant p53. Cancer Res. 2015 Sep 15;75(18):3842-52.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.7698 mL
- 18.8491 mL
- 37.6981 mL
- 5 mM
- 0.7540 mL
- 3.7698 mL
- 7.5396 mL
- 10 mM
- 0.3770 mL
- 1.8849 mL
- 3.7698 mL

技术信息

CAS号

803647-40-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H15N3O4

运输

蓝冰

分子量

265.27

别名

NSC 59984

溶解度

DMSO	93.0 mg/mL (350.6 mM)
Water	37.0 mg/mL (139.5 mM)

动物实验配方

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