Pifithrin-α hydrobromide

Name: Pifithrin-α hydrobromide
Brand: Tocris Bioscience
SKU: 1267
Rating: 5 (3 reviews)

Cat. No. 1267 4 Citations 3 Reviews Submit a Review Datasheet / COA / SDS

Pricing	Availability		Qty

Description: p53 inhibitor. Also aryl hydrocarbon receptor agonist

Chemical Name: 1-(4-Methylphenyl)-2-(4,5,6,7-tetrahydro-2-imino-3(2H)-benzothiazolyl)ethanone hydrobromide

Datasheet

Citations (4)

Reviews (3)

Literature (2)

Pathways (1)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for Pifithrin-α hydrobromide

Pifithrin-α hydrobromide 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 cancer 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). Cyclic analog available (Cat. No. 3843).

Technical Data for Pifithrin-α hydrobromide

M. Wt	367.3
Formula	C₁₆H₁₈N₂OS.HBr
Storage	Desiccate at -20°C
CAS Number	63208-82-2
PubChem ID	9929138
InChI Key	HAGVCKULCLQGRF-UHFFFAOYSA-N
Smiles	Br.CC1=CC=C(C=C1)C(=O)CN1C(=N)SC2=C1CCCC2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Pifithrin-α hydrobromide

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	36.73	100

Preparing Stock Solutions for Pifithrin-α hydrobromide

The following data is based on the product molecular weight 367.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.72 mL	13.61 mL	27.23 mL
5 mM	0.54 mL	2.72 mL	5.45 mL
10 mM	0.27 mL	1.36 mL	2.72 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

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Product Datasheets for Pifithrin-α hydrobromide

Certificate of Analysis / Product Datasheet

Safety Datasheet

References for Pifithrin-α hydrobromide

References are publications that support the biological activity of the product.

Culmsee et al (2001) A synthetic inhibitor of p53 protects neurons against death induced by ischemic and excitotoxic insults, and amyloid β-peptide. J.Neurochem. 77 220 PMID: 11279278

Hoagland et al (2005) The p53 inhibitor pifithrin-α is a potent agonist of the aryl hydrocarbon receptor. J.Pharmacol.Exp.Ther. 314 603 PMID: 15843497

Komarov et al (1999) A chemical inhibitor of p53 that protects mice from the side effects of cancer therapy. Science 285 1733 PMID: 10481009

Komarova and Gudkov (2000) Suppression of p53: a new approach to overcome side effects of antitumor therapy. Biochemistry 65 41 PMID: 10702639

Abdelalim and Tooyama (2012) The p53 inhibitor, pifithrin-α, suppresses self-renewal of embryonic stem cells. Biochem.Biophys.Res.Comm. 420 605 PMID: 22445757

If you know of a relevant reference for Pifithrin-α hydrobromide, please let us know.

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Keywords: Pifithrin-a hydrobromide, Pifithrin-a hydrobromide supplier, p53, inhibitors, inhibits, aryl, hydrocarbon, receptors, agonists, AHR, Transcription, Factors, Pifithrin-alpha, hydrobromide, Aryl, Hydrocarbon, Receptors, Stem, Cell, Signaling, Autophagy, 1267, Tocris Bioscience

4 Citations for Pifithrin-α hydrobromide

Citations are publications that use Tocris products. Selected citations for Pifithrin-α hydrobromide include:

Fraser et al (2006) Regulation of p53 and suppression of apoptosis by the soluble guanylyl cyclase/cGMP pathway in human ovarian cancer cells. Cell Commun Signal 25 2203 PMID: 16288207

Norlin et al (2018) The ATPase activity of Asna1/TRC40 is required for pancreatic progenitor cell survival. Development 145 PMID: 29180572

Li et al (2018) Zinc deficiency causes neural tube defects through attenuation of p53 ubiquitylation. Development 145 PMID: 30545932

Guha et al (2015) Novel Pactamycin Analogs Induce p53 Dependent Cell-Cycle Arrest at S-Phase in Human Head and Neck Squamous Cell Carcinoma (HNSCC) Cells. PLoS One 10 e0125322 PMID: 25938491

Do you know of a great paper that uses Pifithrin-α hydrobromide from Tocris? Please let us know.

Reviews for Pifithrin-α hydrobromide

Average Rating: 5 (Based on 3 Reviews.)

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Study of the effects of p53 inhibition in chemotherapy-induced apoptosis of human cancer cells..

By MARINA KOUTSIOUMPA on 06/10/2021

Assay Type: In Vitro

Species: Human

The inhibitor worked nicely, and the results were consistent. We are happy with the quality of the product.

Pifithrin-alpha.

By Anonymous on 07/12/2020

Assay Type: In Vivo

Species: Mouse

Cell Line/Tissue: neural cell

Pifithrin-alpha were dissolved in DMSO and used at a final concentration of 40 µM for pifithrin-alpha according to previous studies in which 3-100 µM pifithrin-alpha.

PMID: 30545932

The effect of p53 loss in human lung cancer cell lines..

By Anonymous on 01/04/2018

Assay Type: In Vitro

Species: Human

We used the p53 inhibitor in order to tackle the p53 protein in-vitro for some cellular proliferation assays,

We are happy with the quality of the product and the assistance from the Tocris technical department. All our questions about the use of the product where answered within a few hours.

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cell Cycle and DNA Damage Research Product Guide

This product guide provides a review of the cell cycle and DNA damage research area and lists over 150 products, including research tools for:

Cell Cycle and Mitosis
DNA Damage Repair
Targeted Protein Degradation
Ubiquitin Proteasome Pathway
Chemotherapy Targets

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Pathways for Pifithrin-α hydrobromide

p53 Signaling Pathway

p53 signaling plays an important role in the co-ordination of the cellular response different types of stress such as DNA damage and hypoxia. The downstream signals lead to apoptosis, senescence and cell cycle arrest.