Pifithrin-α (PFTα) HBr

For research use only.

Catalog No.S2929

87 publications

Pifithrin-α (PFTα) HBr Chemical Structure

CAS No. 63208-82-2

Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).

Selleck's Pifithrin-α (PFTα) HBr has been cited by 87 publications

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Biological Activity

Description Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes. Pifithrin-α is also a potent agonist of the aryl hydrocarbon receptor (AhR).
p53 [1]
In vitro

Pifithrin-α inhibits p53-dependent transactivation of p53-responsive genes in ConA cells. Pifithrin-α (10 μM) inhibits apoptotic death of C8 cells induced by Dox, etoposide, Taxol, cytosine arabinoside. Pifithrin-α inhibits p53-dependent growth arrest of human diploid fibroblasts in response to DNA damage but has no effect on p53-deficient fibroblasts. Pifithrin-α may modulate the nuclear import or export (or both) of p53 or may decrease the stability of nuclear p53. [1] Pifithrin-α (100-200 nM) completely suppresses the camptothecin-induced increase in the level of p53 DNA binding as well as the p53-responsive gene Bax in hippocampal cell. Pifithrin-α also decreases the basal level of p53 DNA-binding activity. Pifithrin-α (200 nM) protects cultured hippocampal neurons against death induced by DNA-damaging agents. Pifithrin-α (200 μM) stabilizes mitochondrial function, suppresses caspase activation and protects cultured hippocampal neurons against death induced by glutamate and amyloid β-peptide. [2] Pifithrin α, in addition to p53, can suppress heat shock and glucocorticoid receptor signaling but has no effect on nuclear factor-kappaB signaling. Pifithrin α (10 μM) reduces activation of heat shock transcription factor (HSF1) and increases cell sensitivity to heat. Pifithrin α (10 μM) reduces activation of glucocorticoid receptor and rescues mouse thymocytes from apoptotic death after dexamethasone treatment in HeLa cells. [3] PFTalpha blocks p53-mediated induction of p21/Waf-1 in human embryonic kidney cells. PFTalpha does, however, cause a left shift in the dexamethasone dose response curve by increasing intracellular dexamethasone concentration. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse E15.5 cortical neurones NIS4PY1HfW6ldHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGW2b4Dvd4ll\S2rbnT1Z4VlKGSnYYToJI9nKG2xdYPlJGUyPS53IHPvdpRq[2GuIH7leZJwdmW| M3H5bFE3PzV7MUC2

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p53 / p-PKCα / PKCα; 

PubMed: 26733200     

Western blotting analyses of p53 and PKCα (p-PKCα) in MKN45 cells overexpressing p8 treated with the p53 inhibitor PFTα (0–30 μm) for 24 h. Data are mean ± S.D. (n = 3). *, p < 0.05. 

AMPK / p-AMPK / p-ACC / p27 / p53 ; 

PubMed: 21811093     

Protein gel blot analysis of the AMPK/mTOR signaling molecules in SiHa and A549 cells in the presence or absence of PFTα. Phosphorylation of AMPK (P-AMPK) and ACC (P-ACC) and upregulated p27 expression were detected in cells exposed to 20 µM PFTα for 24 h, compared with that in the nontreated control cells. The blots depicted are representative of three independent experiments with similar results.


PubMed: 25862488     

Pifithrin-α was used to inhibit p53 in the SH-SY5Y, SH-EP and WAC(2) cells. Cell lines were treated with pifithrin-α (25 μM) for 48 hours and cell lysates examined for FAK and p53. In all three cell lines there was a decrease in p53 expression following pifithrin-α treatment, and an increase in FAK. Densitometry was performed on all of the blots and verified that p53 and FAK expression were inversely correlated.

26733200 21811093 25862488

PubMed: 26733200     

Immunofluorescence analyses of autophagy (LC3B expression, red) in MKN45 cells overexpressing p8 treated with PFTα (30 μm) for 24 h or left untreated. The nuclei were counterstained with DAPI (blue). Scale bars = 30 μm. 

LC3 / p-AMPK / p27; 

PubMed: 21811093     

Representative images of immunofluorescence staining with anti-P-AMPK and anti-p27 antibodies in GFP-LC3-transfected SiHa cells with or without p53 inhibitor treatment. SiHa cells were transiently transfected with GFP-LC3 plasmids prior to treatment with 20 µM PFTα for 24 h and then immunofluorescently stained as described. scale bar, 10 µm.

26733200 21811093
In vivo Pifithrin-α (2.2 mg/kg i.p.) treatment completely rescues mice (C57BL and Balb/c) of both strains from 60% killing doses of gamma irradiation (8 Gy for C57BL and 6 Gy for Balb/c). Pifithrin-α-injected mice lost less weight than irradiated mice that are not pretreated with the Pifithrin-α. Pifithrin-α (2.2 mg/kg) abrogates p53-dependent regulation of DNA replication after whole-body gamma irradiation in mice. [1] Pifithrin-α (2 mg/kg i.p.) 30 min prior to middle cerebral artery occlusion treatment of mice reduces ischemic brain injury and protects hippocampal neurons against excitotoxic injury. [2] Pifithrin α (3.6 μg/kg i.p.) inhibits Dex-induced degeneration of the thymus in mice. [3] Pifithrin α (2 mg/kg) results in a significantly lower degree of motor disability in rats receiving transient occlusion of the middle cerebral artery as compared with controls. Pifithrin α-treated animals has less motor disability and smaller infarcts when the drug is administered up to an hour after stroke onset. Pifithrin α results in significantly lower motor disability scores in rats than in the vehicle-treated animals at 7 days post-op. Pifithrin α results in significant reduction of apoptosis in rats as indicated by Tunel and caspase 3 staining. [5]


Cell Research:[3]
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  • Cell lines: HCT116 and Hela cells
  • Concentrations: ~10 μM
  • Incubation Time: 48 hours
  • Method: At the end of cell treatments, the number of attached cells is estimated by staining with 0.25% crystal violet in 50% methanol, followed by elution of the dye with 1% SDS. Optical density (530 nm) reflecting the number of stained cells is determined with a Bio-Tek EL311 microplate reader. Cell viability in suspension of short term culture of primary thymocytes is determined by their staining with 0.1% of methyl blue and microscopic counting of blue (dead) cells.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: C57BL and Balb/c mice
  • Dosages: 2.2 mg/kg
  • Administration: Intraperitoneal injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 67 mg/mL (182.41 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+ 40% PEG 300+ 5%Tween80+ 50%ddH2O
For best results, use promptly after mixing.
3.65 mg/ml

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 367.3


CAS No. 63208-82-2
Storage powder
in solvent
Synonyms N/A
Smiles CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br

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p53 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID