Cayman pH-002

pH-002 is an inhibitor of the interaction between the amino- and carboxy-terminal domains of apolipoprotein E4 (ApoE4; IC₅₀ = 116 nM in a FRET reporter assay for domain interaction).^, It restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T, a mutation that impairs ApoE4 domain interactions, when used at a concentration of 100 nM. pH-002 also prevents impairments in neurite outgrowth and dendritic spine development induced by expression of ApoE4 in Neuro-2a cells. It restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC₅₀ = 39 nM) and increases mitochondrial motility in PC12 cells expressing ApoE4 (EC₅₀ = <1 nM).

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