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Pifithrin-β hydrobromide

Pifithrin-β hydrobromide
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).
Catalog No. T3637Cas No. 511296-88-1
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Purity:99.74%
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Pifithrin-β hydrobromide

Catalog No. T3637Cas No. 511296-88-1
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).
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Pack SizePriceAvailabilityQuantity
2 mg$34In Stock
5 mg$51In Stock
10 mg$85In Stock
25 mg$153In Stock
50 mg$223In Stock
100 mg$332In Stock
1 mL x 10 mM (in DMSO)$53In Stock
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Product Introduction

Bioactivity
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.
AliasCyclic PFT-α, PFT-β, Cyclic Pifithrin-α hydrobromide, Pifithrin-β, PFT β (hydrobromide)
Chemical Properties
Molecular Weight349.29
FormulaC16H17BrN2S
Cas No.511296-88-1
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.8630 mL14.3148 mL28.6295 mL143.1475 mL
5 mM0.5726 mL2.8630 mL5.7259 mL28.6295 mL
10 mM0.2863 mL1.4315 mL2.8630 mL14.3148 mL
20 mM0.1431 mL0.7157 mL1.4315 mL7.1574 mL

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