| 应用 |
An inhibitor of p53 that reversibly blocks p53 dependent transcriptional activation and apoptosis. |
| 产品介绍 |
Pifithrin-α (PFTα)是一种p53抑制剂，抑制p53依赖性的p53应答基因转录。 |
| 备注 |
Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. |
| 生化机理 |
Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. It enhances cell survival after genotoxic stress such as UV irradiation and treatment with cytotoxic compounds including doxorubicin , etopoxide, paclitaxel, and cytosine-β-D-arabinofuranoside. Pifithrin-α protects mice from lethal whole body γ-irradiation, and does not induce visible tumors. Protects against neuronal death in models of stroke and neurodegenerative disorders. Pifithrin-α is also an aryl hydrocarbon receptor (AHR) agonist, which leads to the upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM). |
| 别名 |
皮斐松;Pifithrin-α hydrobromide;Pifithrin hydrobromide; Pifithrin-(alpha) hydrobromide; PFT(alpha) hydrobromide;1-(4-Methylphenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)ethanone hydrobromide |
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