PH-002

PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells that could rescue impairments of mitochondrial motility and neurite outgrowth.

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

116 nM (Apo E4 in FRET)[1].

PH-002 is an inhibitor of apolipoprotein (apo) E4 intramolecular domain interaction in neuronal cells, with an IC50 of 116 nM in FRET[1].

PH-002 is also shown to increase COX1 levels in primary neurons from NSE-apoE4 transgenic mouse cortex and hippocampus. After 4 days of treatment with PH-002 (200 nM), COX1 levels are increased by ~60%. PH-002 (100 nM) increases dendritic spine development in primary neurons from NSE-apoE4 transgenic mice to levels comparable with those in NSE-apoE3 primary neurons (apoE3-expressing primary neurons treated with PH-002 gave results identical to untreated primary neurons)[2].

Neuro-2a cells stably expressing apoE3 or apoE4 are seeded at 7500-8000 cells/well on PLlysine-coated 24-well plates containing Opti-MEM with either 0.03% DMSO (control) or DMSO plus compound PH-002 (100 nM)[1].

[1]. Brodbeck J, et al. Structure-dependent impairment of intracellular apolipoprotein E4 trafficking and its detrimental effects are rescued by small-molecule structure correctors. J Biol Chem. 2011 May 13;286(19):17217-26.

[2]. Chen HK, et al. Small molecule structure correctors abolish detrimental effects of apolipoprotein E4 in cultured neurons. J Biol Chem. 2012 Feb 17;287(8):5253-66.

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