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].
Pifithrin-α HBr 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
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