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Pifithrin-α HBr

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Chemical Structure| 63208-82-2 同义名 : Pifithrin hydrobromide;PFTα hydrobromide;PFT-alpha;Pifithrin-alpha;PFT-α;Pifithrin-α;Pifithrin-α hydrobromide
CAS号 : 63208-82-2
货号 : A201732
分子式 : C16H19BrN2OS
纯度 : 98%
分子量 : 367.304
MDL号 : MFCD00417851
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(136.13 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(2.72 mM)，配合低频超声助溶
动物实验配方：

IP 2% DMSO+water 2 mg/mL clear

PO 0.5% CMC-Na 30 mg/mL suspension

生物活性
靶点

  • p53
描述 P53 is known as a transcription factor to control apoptotic cell death through regulating a series of target genes in nucleus[3]. Pifithrin-α hydrobromide is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis[4]. Pifithrin-α also acts as an aryl hydrocarbon receptor (AhR) agonist and. Pifithrin-α is a potent AhR agonist as determined by its ability to bind the AhR, induce formation of its DNA binding complex, activate reporter activity, and up-regulate the classic AhR target gene CYP1A1[5]. When the experiment is performed with Pifthirin-α (PFT-α) hydrobromide, a pharmacological p53 inhibitor, the percentage of annexin V-positive Foxe3-/- SMCs decreases to WT levels. Pifithrin-α (2.2 mg/kg, i.p.) significantly reduces the incidence of aortic rupture and intramural hematomas in Foxe3-/- mice that underwent transverse aortic constriction (TAC) (50% to 17%, P<0.05). After Pifthirin-α treatment, the mean diameter of the ascending aorta and the percentage of TUNEL-positive cells in the aortic media are also normalized to WT levels in surviving Foxe3-/- animals[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
mouse E15.5 cortical neurones Function assay Inhibition of etoposide-induced death of mouse E15.5 cortical neurones 16759106
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.61mL

2.72mL

1.36mL

27.23mL

5.45mL

2.72mL
参考文献

[1]Yu W, Zhang X, Liu J, et al. Cyclosporine A Suppressed Glucose Oxidase Induced P53 Mitochondrial Translocation and Hepatic Cell Apoptosis through Blocking Mitochondrial Permeability Transition. Int J Biol Sci. 2016;12(2):198-209.

[2]Komarov PG, Komarova EA, Kondratov RV, et al. A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science. 1999;285(5434):1733-1737.

[3]Hoagland MS, Hoagland EM, Swanson HI. The p53 inhibitor pifithrin-alpha is a potent agonist of the aryl hydrocarbon receptor. J Pharmacol Exp Ther. 2005;314(2):603-610.

[4]Kuang SQ, Medina-Martinez O, Guo DC, et al. FOXE3 mutations predispose to thoracic aortic aneurysms and dissections. J Clin Invest. 2016;126(3):948-961.