Pifithrin-α (PFTα) HBr
Molecular Weight(MW): 367.3
Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.
Cited by 7 Publications
3 Customer Reviews
(C) Cell viability was measured after TSA and PFTα co-treatment. MG63 were exposed to TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment compared with TSA treatment alone for 24h. Data are presented as means ± S.E.M. from 3 independent experiments. *, P < 0.05 vs. MG63 cells without TSA or PFTα treatment; **, P < 0.01 vs. MG 63 cells without TSA or PFTα treatment; &&, P < 0.01 vs. MG63 cells with TSA treatment alone. (D) Flow cytometry analysis of ANXA5 and propidiumiodide staining of MG63 cells with TSA and various concentrations of PFTα (1, 5, 10μM) co-treatment, compared with TSA treatment alone.
Int J Biol Sci, 2016, 12(11):1298-1308. Pifithrin-α (PFTα) HBr purchased from Selleck.
A, HAECs were per-incubated with PFTα (3 μmol/L) for 60 min followed by transfected with siB-myb or siNC in the presence of PFTα (3 μmol/L) for 7 d. The expression levels of B-myb, p-p53, p53 and p21 proteins were analysed by western blotting. GAPDH was used as a loading control. A typical group of blots is shown from one of three independent experiments.
Cell Prolif, 2017. Pifithrin-α (PFTα) HBr purchased from Selleck.
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|Description||Pifithrin-α is an inhibitor of p53, inhibiting p53-dependent transactivation of p53-responsive genes.|
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.  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.  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.  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. 
|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.  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.  Pifithrin α (3.6 μg/kg i.p.) inhibits Dex-induced degeneration of the thymus in mice.  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. |
-  Komarov PG, et al. Science, 1999, 285(5434), 1733-1737.
-  Culmsee C, et al. J Neurochem, 2001, 77(1), 220-228.
-  Komarova EA, et al. J Biol Chem, 2003, 278(18), 15465-15468.
|In vitro||DMSO||67 mg/mL (182.41 mM)|
|In vivo||Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
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