[Taiclone] Pifithrin-μ

[Taiclone] Pifithrin-μ

 

tcsc0002901

 

CAS No

64984-31-2

 

Formula

C8H7NO2S

 

Clinical Information

clinical

information

 

Pathway

Metabolic Enzyme/Protease
Cell Cycle/DNA Damage
Apoptosis

 

Target

HSP
HSP
MDM-2/p53

 

Purity / Grade

>98%

 

Solubility

DMSO : ≥ 108 mg/mL (595.99 mM)

 

Smiles

smiles

 

Alternative Names

PFTμ;2-Phenylethynesulfonamide

 

Observed Molecular Weight

181.21

 

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].