EasySep™小鼠TIL（CD45）正选试剂盒
产品号 #72062_C
p53抑制剂
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总览
环状Pifthrin-Alpha是一种可渗透细胞且可逆的p53介导的细胞凋亡和p53依赖性基因转录抑制剂。它是非环状Pifithrin-Alpha的更稳定且细胞毒性更低的类似物。据报道，环状Pifithrin-Alpha还可激活芳烃受体（Fernandez-Cruz et al., Gary & Jensen, Komarov et al.）。
重编程
·提高小鼠胚胎成纤维细胞重编程为诱导多能干细胞的效率（Liao et al.）。
维持和自我更新
·降低紫外线诱导的小鼠胚胎干细胞凋亡（Qin et al.）。
·增加小鼠体内和体外造血干细胞和祖细胞的数量，并降低辐射诱导的这些细胞死亡（Leonova et al.）。
别名
环状PFT-α，环状Pifithrin-α，PFT-β，Pifithrin-β
细胞类型
造血干/祖细胞，多能干细胞
种属
人，小鼠，非人灵长类，其他物种，大鼠
应用
扩增，培养，重编程
研究领域
干细胞生物学
CAS 编号
511296-88-1
化学式
C₁₆H₁₆N₂S · HBr
分子量
349.3 g/mol
纯度
≥ 95 %
通路
p53
靶点
p53
产品说明书及文档
请在《产品说明书》中查找相关支持信息和使用说明，或浏览下方更多实验方案。
应用领域
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相关材料与文献
技术资料 (3)
文献 (6)
A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy.
Science (New York,N.Y.) 1999 SEP
Abstract
Chemotherapy and radiation therapy for cancer often have severe side effects that limit their efficacy. Because these effects are in part determined by p53-mediated apoptosis,temporary suppression of p53 has been suggested as a therapeutic strategy to prevent damage of normal tissues during treatment of p53-deficient tumors. To test this possibility,a small molecule was isolated for its ability to reversibly block p53-dependent transcriptional activation and apoptosis. This compound,pifithrin-alpha,protected mice from the lethal genotoxic stress associated with anticancer treatment without promoting the formation of tumors. Thus,inhibitors of p53 may be useful drugs for reducing the side effects of cancer therapy and other types of stress associated with p53 induction.
The p53 inhibitor pifithrin-alpha forms a sparingly soluble derivative via intramolecular cyclization under physiological conditions.
Molecular pharmaceutics JAN
Abstract
The transcription factor p53 coordinates cell cycle arrest and apoptosis in response to DNA damage. Pifithrin-alpha (PFT-alpha) is a small molecule inhibitor of p53 activity that is frequently used in cell culture studies of p53 function. Here we report an investigation of the stability of this compound. PFT-alpha rapidly converts to a planar tricyclic derivative,with a half-life of 4.2 h under physiological conditions. This spontaneous conversion greatly alters the structural and physicochemical properties of the drug. PFT-alpha has a pKa of 9.11 and is an ionic species in physiological medium,whereas the tricyclic derivative has a pKa of 4.36 and exists as the neutral free base at pH 7. The tricyclic derivative is very hydrophobic,with a log P of 4.26. Although PFT-alpha is generally used at 10-30 microM concentration,the aqueous solubility of its derivative is only 0.2 microM,and it can form a visible precipitate under conditions of typical use. The conversion of PFT-alpha proceeds via an intramolecular cyclization reaction involving the imine and carbonyl groups. Modification of the carbonyl function creates a stable analogue of PFT-alpha that remains soluble indefinitely. These results provide a strategy for the rational design of PFT-alpha analogues that exhibit predictable stability,hydrophobicity,and aqueous solubility.
Regulation of apoptosis and differentiation by p53 in human embryonic stem cells.
The Journal of biological chemistry 2007 FEB
Abstract
The essentially infinite expansion potential and pluripotency of human embryonic stem cells (hESCs) makes them attractive for cell-based therapeutics. In contrast to mouse embryonic stem cells (mESCs),hESCs normally undergo high rates of spontaneous apoptosis and differentiation,making them difficult to maintain in culture. Here we demonstrate that p53 protein accumulates in apoptotic hESCs induced by agents that damage DNA. However,despite the accumulation of p53,it nevertheless fails to activate the transcription of its target genes. This inability of p53 to activate its target genes has not been observed in other cell types,including mESCs. We further demonstrate that p53 induces apoptosis of hESCs through a mitochondrial pathway. Reducing p53 expression in hESCs in turn reduces both DNA damage-induced apoptosis as well as spontaneous apoptosis. Reducing p53 expression also reduces spontaneous differentiation and slows the differentiation rate of hESCs. Our studies reveal the important roles of p53 as a critical mediator of human embryonic stem cells survival and differentiation.
更多信息
| Molecular Weight | 349.3 g/mol |
|---|---|
| 物种 | 人, 其它物种, 大鼠, 小鼠, 非人灵长类 |
| Alternative Names | Cyclic PFT-α, Cyclic Pifithrin-α, PFT-β, Pifithrin-β |
| Cas Number | 511296-88-1 |
| Chemical Formula | C₁₆H₁₆N₂S · HBr |
| 纯度 | ≥ 95 % |
| Target | p53 |
| Pathway | p53 |
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质量保证:
产品仅供研究使用，不用于针对人或动物的诊断或治疗。
产品仅供研究使用，不用于针对人或动物的诊断或治疗。
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