PH-002, an inhibitor targeting the intramolecular domain interaction of apolipoprotein (apo) E4 in neuronal cells, additionally enhances mitochondrial motility and promotes neurite outgrowth, thereby countering related impairments.

ApoE4 (FRET):116 nM

PH-002 inhibits intramolecular domain interaction of apolipoprotein (apo) E4 in neuronal cells (IC50: 116 nM in FRET) [1].

PH-002 (100 nM) promotes dendritic spine development in primary neurons from NSE-apoE4 transgenic mice to levels similar to those in NSE-apoE3 neurons (apoE3-expressing primary neurons treated with PH-002 show results comparable to untreated neurons). Additionally, PH-002 enhances COX1 levels in primary neurons from the NSE-apoE4 transgenic mouse cortex and hippocampus, increasing COX1 by ~60% after 4 days of treatment at 200 nM [2].