1. Apoptosis
    Metabolic Enzyme/Protease
    Cell Cycle/DNA Damage
  2. MDM-2/p53
    HSP

Pifithrin-μ (Synonyms: PFTμ; 2-Phenylethynesulfonamide)

Cat. No.: HY-10940
Handling Instructions

Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

For research use only. We do not sell to patients.
Pifithrin-μ Chemical Structure

Pifithrin-μ Chemical Structure

CAS No. : 64984-31-2

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.

IC50 & Target

p53[1], HSP70[2]

In Vitro

Pifithrin-μ (10 μM) is a p53 inhibitor, which inhibits p53 binding to mitochondria by reducing its affinity to antiapoptotic proteins Bcl-xL and Bcl-2 but has no effect on p53-dependent transactivation, activity of caspases 2, 8, 9 and 10 in a cell-free system, or NF-κB-dependent transcription[1]. Pifithrin-μ (PES) time- and dose-dependently reduces viability in A549 cells, with IC50s of 44.9 and 25.7 µM at 24 h and 48 h. Pifithrin-μ (20 μM) suppresses the cell migration, induces cell cycle arrest and cell apoptosis in A549 and H460 cells. Pifithrin-μ (10 or 20 µM) inhibits activities of AKT, ERK, and Hsp70 in A549 and H460 cells. Pifithrin-μ (20 µM) sensitizes A549 and H460 cell lines to TRAIL-induced cell proliferation inhibition and apoptosis[2].

In Vivo

Pifithrin-μ (40 mg/kg, i.p.) shows no protective effect against doses of radiation that cause gastrointestinal syndrome in mice[1]. Pifithrin-μ (PES, 10 mg/kg) shows antitumor effect in mice bearing A549 cells[2]. Pifithrin-μ exhibits neuroprotective effect with the P53-inhibitor pifithrin-μ after cardiac arrest in a rodent model[3].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 5.5185 mL 27.5923 mL 55.1846 mL
5 mM 1.1037 mL 5.5185 mL 11.0369 mL
10 mM 0.5518 mL 2.7592 mL 5.5185 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[2]

Pifithrin-μ is dissolved in DMSO[2].

The cell viability is determined by the Cell Counting Kit-8 assay. Briefly, A549 and H460 cells are incubated in 96-well plates at a density of 5 × 103 per 100 µL of culture medium overnight. After treated with indicated concentration of Pifithrin-μ for 24 and 48 h, 10 µL of tetrazolium substrate are added to each well of the plate. After incubation at 37°C for 1 h, the absorbance is recorded at a wavelength of 450 nm using a microplate reader. Each experiment is determined in triplicate and repeated at least three times[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Pifithrin-μ is formulated in PBS[2].

Mice[2]
A549 cells (1 × 107) are suspended in Matrigel and inoculated subcutaneously into the mice. Twelve mice bearing evident tumors are arbitrarily assigned to PBS control group and Pifithrin-μ treatment groups (six mice per group). When tumors reach a size of ∼5×5 mm2, mice are treated with either a single of intraperitoneal injection of Pifithrin-μ (20 mg/kg) or PBS every two days. After 3-week treatment, mice are euthanized with carbon dioxide. Tumor burdens are evaluated by measuring body weight, tumor weight, and tumor volume. Tumor volume is determined as 0.5 × length × width2. Tumor samples are collected and fixed in 10% neutral buffered formalin. Hematoxylin and eosin staining and immunohistochemistry for histological analysis of tumor samples are measured[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

181.21

Formula

C₈H₇NO₂S

CAS No.

64984-31-2

SMILES

O=S(C#CC1=CC=CC=C1)(N)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Pifithrin-μ
Cat. No.:
HY-10940
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