Home Apoptosis p53 inhibitor - Autophagy activator - AhR agonist Pifithrin-α (PFTα) HBr For research use only.

Pifithrin-α (PFTα) HBr

Synonyms: Pifithrin-α hydrobromide

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

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

Batch: Purity: 99.87%
99.87

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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 FAK AMPK / p-AMPK / p-ACC / p27 / p53 p53 / p-PKCα / PKCα 25862488
Immunofluorescence LC3 / p-AMPK / p27 LC3B 21811093
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

Chemical lnformation & 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)

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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