Pifithrin-? has been used:to treat microglial cell line to analyse its neuroprotective effect on M1-like and M2-like phenotypeas heat shock protein (HSP)-70 inhibitor, to treat transfected Marc-145 cellsto inhibit heat shock cognate 70 (Hsc70) to elucidate heat shock chaperones mouse embryonic stem cells
Biochem/physiol Actions
Pifithrin-µ is an inhibitor of p53 binding and anti-apoptotic, which directly inhibits p53 binding to mitochondria as well as to Bcl-xL and Bcl-2 proteins. PFTµ rescues cells from lethal γ-irradiation-induced cell death. Because pifithrin-µ shuts down only the p53-mitochondrial pathway without affecting the transcriptional functions of p53, it is superior to pifithrin-α.
Pifithrin-?(PFT-?) has neuroprotective capabilities against cell death in a preclinical model of hypoxia-ischemia (HI)-induced neonatal encephalopathy. It inhibits nuclear factor-?B (NF-?B) pathway by inhibiting the interaction of molecular chaperone heat shock protein (HSP)-70 with its substrates.