NSC-59984

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种小分子，可破坏癌细胞中突变型 p53 的稳定性并恢复野生型 p53 通路。

A small molecule that both destabilize mutant p53 and restores wild-type p53 pathway in cancer cells; induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway, restores wild-type p53 signaling via p73 activation, specifically in mutant p53-expressing colorectal cancer cells. degrades mutant p53R273H, rescued CDH6 expression; significantly represses DLD-1 xenograft tumor growth.

NSC59984 specifically restores p53 pathway signaling in mutant p53-expressing human colorectal cancer cells. NSC59984 induces cell death in tumor cells but not normal cells with little or no genotoxicity. NSC59984 induces mutant p53 protein degradation through MDM2-mediated ubiquitination in cancer cells. NSC59984 restores p53 pathway signaling through activation of p73. NSC59984 induces p73-dependent cell apoptosis in cancer. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 μM for p53-null HCT116 cells.

NSC59984 synergizes with CPT11 to induce cell death in mutant p53-expressing colorectal cancer cells and inhibits mutant p53-associated colon tumor xenograft growth in a p73-dependent manner.

NSC 59984 | NSC59984

Apoptosis

MDM2-p53

p53

Cancer

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803647-40-7

265.2652

C12H15N3O4

>98% (HPLC)

DMSO: ≥ 38 mg/mL

O=C(N1CCN(C)CC1)/C=C/C2=CC=C([N+]([O-])=O)O2

2-Propen-1-one, 1-(4-methyl-1-piperazinyl)-3-(5-nitro-2-furanyl)-

(-20℃)

With Ice Pack

≥ 2 years