NSC59984
产品编号: DC9257
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应用领域
NSC59984 通过 MDM2 和泛素-蛋白酶体途径而诱导突变型 p53 蛋白降解。NSC59984 靶向 GOF 突变体 p53,并刺激 p73 恢复 p53 途径的信号传导。
Cas No.: |
803647-40-7 |
名称: |
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别名: |
NSC-59984,NSC 59984 |
SMILES: |
CN1CCN(CC1)C(=O)/C=C/C2=CC=C(O2)[N+](=O)[O-] |
分子式: |
C12H15N3O4 |
分子量: |
265.27 |
纯度: |
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保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: |
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In Vivo: |
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In Vitro: |
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References: |
NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. 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.
in vitro: 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.
in vivo: 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. |
Kinase Assay: |
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Cell Assay: |
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Animal Administration: |
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References: |
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MSDS
COA
LOT NO. |
DOWNLOAD |
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2018-0101 |
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