Pifithrin-μ

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

Product information

CAS Number: 64984-31-2

Molecular Weight: 181.21

Formula: C8H7NO2S

Synonym:

PFTμ

2-Phenylethynesulfonamide

Chemical Name: phenylethynesulfonamide

Smiles: NS(=O)(=O)C#CC1C=CC=CC=1

InChiKey: ZZUZYEMRHCMVTB-UHFFFAOYSA-N

InChi: InChI=1S/C8H7NO2S/c9-12(10,11)7-6-8-4-2-1-3-5-8/h1-5H,(H2,9,10,11)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 108 mg/mL (595.99 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

In Vivo:

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

References:

1. Strom E, et al. Small-molecule inhibitor of p53 binding to mitochondria protects mice from gamma radiation. Nat Chem Biol. 2006 Sep;2(9):474-9. Epub 2006 Jul 23.
2. Zhou Y, et al. Pifithrin-μ is efficacious against non-small cell lung cancer via inhibition of heat shock protein 70. Oncol Rep. 2017 Jan;37(1):313-322.
3. Glas M, et al. Neuroprotection with the P53-Inhibitor Pifithrin-μ after Cardiac Arrest in a Rodent Model. Shock. 2018 Feb;49(2):229-234.

Products are for research use only. Not for human use.