Pifithrin-α Hydrobromide

Cat. No. IC23127

CAS. No. 63208-82-2

Key Features and Details

Category

Inhibitor&Activator

Purity

98.05%

Formula

C16H19BrN2OS

Product Size

Online Inquiry

Product Details

Product Name

Pifithrin-α Hydrobromide

CAS No.

63208-82-2

Molecular Weight

367.30

Synonyms

Pifithrin hydrobromide; PFTα hydrobromide

Formula

C16H19BrN2OS

Appearance

Solid

Purity

98.05%

SMILES

N=C1SC2=C(CCCC2)N1CC(C3=CC=C(C)C=C3)=O.[H]Br

Product Overview

Description

Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.

In Vitro Activity

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 Activity

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 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).

Storage & Handling

Storage

4 °C, sealed storage, away from moisture In solvent : -80 °C, 6 months; -20 °C, 1 month (sealed storage, away from moisture)

Shipping

Room temperature in continental US; may vary elsewhere.

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.