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Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | In Stock | |
5 mg | $51 | In Stock | |
10 mg | $85 | In Stock | |
25 mg | $153 | In Stock | |
50 mg | $223 | In Stock | |
100 mg | $332 | In Stock | |
1 mL x 10 mM (in DMSO) | $53 | In Stock |
Description | Pifithrin-β hydrobromide (Cyclic PFT-α) is an inhibitor of p53; reversibly blocks p53-dependent transcriptional activation and apoptosis. Protects against neuronal death in models of stroke and neurodegenerative disorders. Active in vivo; protects mice from the side-effects of Y therapy associated with p53 induction. Supresses self-renewal of embryonic stem cells. Also aryl hydrocarbon receptor (AHR) agonist, causes upregulation of AHR target gene CYP1A1 (EC50 = 1.1 μM). |
Targets&IC50 | p53:23 μM(EC50) |
In vitro | PFTα molecule could not take a planar conformation required for AhR activation whereas Pifithrin-β hydrobromide showed a conformation similar to those of the prototypical AhR ligand β-naphthoflavone. In both cell lines, PFTα and Pifithrin-β hydrobromide provoked different responses related with AhR activation. However, when cyclization of PFTα to Pifithrin-β hydrobromide was hampered by acetylation of the exocyclic nitrogen, all these responses were not observed. These results lead to the conclusion that the activation of the AhR is probably caused by Pifithrin-β hydrobromide instead of PFTα. |
Alias | Pifithrin-β, PFT-β, PFT β (hydrobromide), Cyclic Pifithrin-α hydrobromide, Cyclic PFT-α |
Molecular Weight | 349.29 |
Formula | C16H17BrN2S |
Cas No. | 511296-88-1 |
Smiles | Br.Cc1ccc(cc1)-c1cn2c3CCCCc3sc2n1 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 13.75 mg/mL (39.37 mM) ![]() | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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