Name: Pifithrin-α (PFTα) HBr
Brand: Selleck Chemicals
SKU: S2929
Rating: 5 (116 reviews)

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).

Pifithrin-α (PFTα) HBr Chemical Structure

CAS: 63208-82-2

Selleck's Pifithrin-α (PFTα) HBr has been cited by 116 publications

Purity & Quality Control

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Signaling Pathway

p53 Signaling Pathway

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
mouse E15.5 cortical neurones	Function assay				Inhibition of etoposide-induced death of mouse E15.5 cortical neurones	16759106
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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).

Targets

p53 ^[1]

In vitro
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 Research	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.
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	p53 / p-PKCα / PKCα AMPK / p-AMPK / p-ACC / p27 / p53 FAK		26733200
	Immunofluorescence	LC3B LC3 / p-AMPK / p27		26733200

In Vivo
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]
Animal Research	Animal Models	C57BL and Balb/c mice
	Dosages	2.2 mg/kg
	Administration	Intraperitoneal injection

References

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Chemical Information & Solubility

Molecular Weight	367.3	Formula	C₁₆H₁₈N₂OS.HBr
CAS No.	63208-82-2	SDF	Download Pifithrin-α (PFTα) HBr SDF
Smiles	CC1=CC=C(C=C1)C(=O)CN2C3=C(CCCC3)SC2=N.Br
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 73 mg/mL ( (198.74 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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