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Chemical Structure| 63208-82-2 Chemical Structure| 63208-82-2

Structure of Pifithrin-α HBr
CAS No.: 63208-82-2

Chemical Structure| 63208-82-2

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Pifithrin-α hydrobromide is a p53 inhibitor that blocks its transcriptional activity and prevents cell apoptosis. Additionally, it acts as an aryl hydrocarbon receptor (AhR) agonist.

Synonyms: Pifithrin hydrobromide; PFTα hydrobromide; PFT-alpha

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Product Details of Pifithrin-α HBr

CAS No. :63208-82-2
Formula : C16H19BrN2OS
M.W : 367.30
SMILES Code : CC1=CC=C(C(CN2C(SC3=C2CCCC3)=N)=O)C=C1.[H]Br
Synonyms :
Pifithrin hydrobromide; PFTα hydrobromide; PFT-alpha
MDL No. :MFCD00417851
InChI Key :HAGVCKULCLQGRF-UHFFFAOYSA-N
Pubchem ID :9929138

Safety of Pifithrin-α HBr

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • p53

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293-OATP1B3 cells 30 µM 5 h To investigate the effect of Pifithrin-α on microcystin-LR-induced cytotoxicity, results showed that Pifithrin-α concentration-dependently attenuated the susceptibility of HEK293-OATP1B3 cells to microcystin-LR. Environ Health Perspect. 2010 Sep;118(9):1292-8.
Human Coronary Artery Smooth Muscle Cells (HCASMC) 10 μM To investigate the effect of Pifithrin-α on the p53 signaling pathway in CDKN2B-deficient cells, results showed that Pifithrin-α inhibited the p53 signaling pathway and reduced apoptosis. Arterioscler Thromb Vasc Biol. 2013 Jan;33(1):e1-e10.
HepG2 cells 20 µM 24 h Inhibition of p53 activation, reduction of caspase-3 cleavage, and significant reduction of OH-ME-induced cell death Cell Death Dis. 2022 Nov 29;13(11):1009.
HK2 cells 10μM 48 h Inhibit p53 protein levels and activity, and evaluate its impact on TGFβ1 mRNA and protein levels as well as mesenchymal transition. The results showed that PFT-α treatment partially reversed the increases in TGFβ1 mRNA and protein levels, as well as the expression of mesenchymal markers α-SMA and Vimentin induced by Bmi1 knockdown or H2O2 treatment, while partially restoring the expression of the epithelial marker E-Cadherin. Int J Biol Sci. 2024 Mar 11;20(6):2008-2026.
A172 cells 10 μM Pifithrin-α (p53 inhibitor) was used to perform the rescue experiment, but the results indicated that pifithrin-α (PFT-a) could not significantly affect the impact of p62 overexpression on SLC7A11 in A172 (p53 wild-type) cells. Cell Biosci. 2022 Feb 25;12(1):20.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Piezo1scKO mouse model Intraperitoneal injection 2 mg/kg Every second day until sample isolation Inhibition of P53 activity, reduction of senescent muscle stem cell formation, and improvement of muscle regeneration Redox Biol. 2022 Jun;52:102309
Mice Carotid Artery Ligation (CAL) model and Elastase-induced Abdominal Aortic Aneurysm (AAA) model Intraperitoneal injection 2.2 mg/kg Every 48 hours until sacrifice To investigate the effect of Pifithrin-α on vascular remodeling and aneurysm formation in Cdkn2b-deficient mice, results showed that Pifithrin-α inhibited the p53 signaling pathway, reduced apoptosis, and reversed the vascular remodeling phenotype. Arterioscler Thromb Vasc Biol. 2013 Jan;33(1):e1-e10.
Mice MYC-induced T-cell acute lymphocytic lymphoma model Intraperitoneal injection 4 mg/kg Thrice weekly for two weeks Inhibit p53 to study its effect on CSC self-renewal Cancer Res. 2019 Aug 15;79(16):4015-4025

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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