Pifithrin-μ

Research use only, not for human use.

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

Pifithrin-μ is an inhibitor of p53-mediated apoptosis. It acts by preventing p53 binding to Bcl-xL and Bcl-2 at the mitochondria without affecting p53 transactivational activities.

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.

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.

Pifithrin-μ | Pifithrin μ | Pifithrinμ

Cell Cycle/DNA Damage

DNA/RNA Synthesis

p53

Cancer

——

64984-31-2

181.21

C8H7NO2S

>98% (HPLC)

DMSO : ≥ 108 mg/mL; 595.99 mM

c1ccc(cc1)C#CS(=O)(=O)N

2-Phenylethynesulfonamide

(-20℃)

With Ice Pack

≥ 2 years