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Pifithrin-β hydrobromide

Catalog No. T3637 CAS 511296-88-1

Synonyms: Cyclic PFT-α, PFT-β, Cyclic Pifithrin-α hydrobromide, Pifithrin-β, PFT 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).

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Pifithrin-β hydrobromide Chemical Structure

Pifithrin-β hydrobromide, CAS 511296-88-1

Pack Size	Availability	Price/USD
2 mg	In stock	$ 34.00
5 mg	In stock	$ 51.00
10 mg	In stock	$ 85.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 223.00
100 mg	In stock	$ 332.00
1 mL * 10 mM (in DMSO)	In stock	$ 53.00

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Purity: 99.62%

Purity: 99.24%

Biological Description

Chemical Properties

Storage & Solubility Information

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 PFTβ showed a conformation similar to those of the prototypical AhR ligand β-naphthoflavone. In both cell lines, PFTα and PFTβ provoked different responses related with AhR activation. However, when cyclization of PFTα to PFTβ 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 PFTβ instead of PFTα.

Synonyms	Cyclic PFT-α, PFT-β, Cyclic Pifithrin-α hydrobromide, Pifithrin-β, PFT β (hydrobromide)
Molecular Weight	349.29
Formula	C16H17BrN2S
CAS No.	511296-88-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 13.75 mg/mL (39.37 mM)

References and Literature

1. Christodoulou MS, et al. Synthesis and biological evaluation of imidazolo[2,1-b]benzothiazole derivatives, as potential p53 inhibitors. Bioorg Med Chem. 2011 Mar 1;19(5):1649-57. 2. Da Pozzo E , La Pietra V , Cosimelli B , et al. p53 Functional Inhibitors Behaving Like Pifithrin-β Counteract the Alzheimer Peptide Non-β-amyloid Component Effects in Human SH-SY5Y Cells[J]. ACS Chemical Neuroscience, 2014, 5(5):390-399. 3. Feng F, Wang Z, Li R, et al. Citrus alkaline extracts prevent fibroblast senescence to ameliorate pulmonary fibrosis via activation of COX-2[J]. Biomedicine & Pharmacotherapy. 2019 Apr;112:108669.

Citations

1. Xu D, Xu Y, Cui Q, et al. Cold atmospheric plasma as a potential tool for multiple myeloma treatment. Oncotarget. 2018, 9(26): 18002 2. Feng F, Wang Z, Li R, et al. Citrus alkaline extracts prevent fibroblast senescence to ameliorate pulmonary fibrosis via activation of COX-2. Biomedicine & Pharmacotherapy. 2019 Apr;112:108669

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Transcription Factor-Targeted Compound Library Pyroptosis Compound Library Apoptosis Compound Library Ferroptosis Compound Library Anti-Lung Cancer Compound Library NO PAINS Compound Library Bioactive Compounds Library Max HIF-1 Signaling Pathway Compound Library Metabolism Compound Library

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Keywords

Pifithrin-β hydrobromide 511296-88-1 Apoptosis Ferroptosis p53 Cyclic PFT-α inhibit PFT-beta Pifithrin-b PFT β Cyclic PFT-a PFT-β MDM-2/p53 PFT-b PFT beta Pifithrinβ hydrobromide Cyclic Pifithrin-a Hydrobromide PFT b Cyclic Pifithrin-α Hydrobromide Pifithrin-b Hydrobromide Pifithrin β hydrobromide Cyclic Pifithrin-α hydrobromide Pifithrin-beta Cyclic Pifithrin-α Inhibitor Pifithrin-β Cyclic Pifithrin-alpha Hydrobromide Cyclic PFT-alpha Pifithrin-beta Hydrobromide PFT β (hydrobromide) Pifithrin-β Hydrobromide inhibitor

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