Pifithrin-μ is a specific small molecule inhibitor of p53 and HSP70, shows antitumor and neuroprotective activity. 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. 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 uM, 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.
Physicochemical Properties
M.Wt
181.21
Formula
C8H7NO2S
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
2-Phenylethyne-1-sulfonamide
References
1. Strom E, et al. Nat Chem Biol. 2006 Sep;2(9):474-9. Epub 2006 Jul 23.
2. Zhou Y, et al. Oncol Rep. 2017 Jan;37(1):313-322.
