Pifithrin-u

Cas No.:	64984-31-2
Chemical Name:	Ethynesulfonamide,2-phenyl-
SMILES:	O=S(C#CC1=CC=CC=C1)(N)=O
Formula:	C8H7NO2S
M.Wt:	181.21
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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