PK11000
产品说明书
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同义名 : | - |
| CAS号 : | 38275-34-2 | |
| 货号 : | A536947 | |
| 分子式 : | C6H5ClN2O4S | |
| 纯度 : | 99% | |
| 分子量 : | 236.63 | |
| MDL号 : | MFCD00507244 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | The tumor suppressor p53 plays a key role in regulating cell cycle arrest, DNA repair, apoptosis, and cell senescence and is inactivated either by mutation or up-regulation of proteins such as MDM2 or MDMX in virtually all human cancers. Cancers with mutant p53 often show increased metastasis, genomic instability, and higher chemoresistance. PK11007, a thiol-modifying compound, exerts antitumor function via reactivating p53. PK11007 increased protein levels of the p53 target genes p21, MDM2, and PUMA in a mostly concentration-dependent manner in NUGC-3 (p53-Y220C), HUH-7 (p53-Y220C) and MKN1 (p53-V143A) cells and also activated the unfolded protein response pathway in a concentration-dependent manner in HUH-7 cells. PK11007 slightly increased caspase 3/7 activity without inducing membrane permeabilization in SW480 (15% increase at 15 μM), SJSA-1 (40% increase at 30 μM), and HCT116 (10% increase at 60 μM) cells, and depleted GSH and increased concentration of ROS[1]. PK11007 was found to induce apoptosis in both a time and concentration-dependent manner in the two p53-mutated triple-negative breast cancer cell lines investigated, HCC1143 and MDA-MB-468, but not in the WT-p53 cell line, MCF-7[2]. | ||
| 作用机制 | PK11007 stabilizes p53 in vitro via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
4.23mL 0.85mL 0.42mL |
21.13mL 4.23mL 2.11mL |
42.26mL 8.45mL 4.23mL |
| 参考文献 |
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