Biochem/physiol Actions Pifithrin-α is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression. Pifithrin-α 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 without an increase in cancer incidence. The protective effect is not seen in p53-null mice or cells expressing a dominant negative mutant of the p53 gene. Protection is conferred by the transient expression of p53 in p53-deficient cell lines.
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生物活性
PubChem BioAssay
化合物性质
产品相关信息
运输包装
wet ice
纯度
≥95% (HPLC)
成盐信息
HBr
理化性质
溶解度
DMSO: soluble20 mg/mL
熔点
192.1-192.5 °C(lit.)
off-white powder
安全信息
Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter