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Pifithrin-α hydrobromide

CAS No. : 63208-82-2

MCE 站：Pifithrin-α hydrobromide

产品活性：Pifithrin-α hydrobromide是 p53 抑制剂，可阻断其转录活性并阻止细胞凋亡。Pifithrin-α hydrobromide 同时为 aryl hydrocarbon receptor (AhR) 的激动剂。

研究领域：Apoptosis  |  Immunology/Inflammation

作用靶点：MDM-2/p53  |  Aryl Hydrocarbon Receptor  |  Ferroptosis

In Vitro: Pifithrin-α (PFT-α) hydrobromideis a water-soluble compound that could suppress p53 protein transcription. Pifithrin-α can suppress glucose oxidase (GOX)-induced p53 protein increase in whole cell lysates, but cyclosporine A (CsA) fails to show such an inhibition effect. Notably, Pifithrin-α is able to block the GOX-induced Bcl-2 protein reduction. Similarly, it is Pifithrin-α rather than CsA that able to prevent the Bax increasing in whole cell lysates. Pifithrin-α inhibits p53-dependent apoptosis through an undetermined mechanism. 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.

In Vivo: 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 (P<0.05).

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