敏感性 | 对光和热敏感 |
溶解性 | Soluble in DMSO (20 mg/ml), water, DMF (~1 mg/ml), 1:10 DMSO:PBS (pH 7.2) (~ 0.1 mg/ml), 100% ethanol, and methanol. Sparingly soluble in aqueous buffers. |
存贮条件 | 储存温度 -20°C,避光保存 |
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 |