An inhibitor of ApoE4 domain interactions (IC50 = 116 nM in a FRET reporter assay for amino- and carboxy-terminal domain interactions); restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T at 100 nM; restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in neurons expressing ApoE4 (EC50 =

PH-002 – 5 mg

Brand:
Cayman
CAS:
1311174-68-1
Storage:
-20
UN-No:
Non-Hazardous - /

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).{43809,51125} 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).{43809}  

 

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SKU: 27739 - 5 mg Category:

Description

An inhibitor of ApoE4 domain interactions (IC50 = 116 nM in a FRET reporter assay for amino- and carboxy-terminal domain interactions); restores intracellular trafficking of ApoE4 to the endoplasmic reticulum and Golgi apparatus in Neuro-2a cells expressing EGFP-ApoE4 or EGFP-ApoE4-R61T at 100 nM; restores levels of mitochondrial complex IV subunit 1 in Neuro-2a cells expressing ApoE4 (EC50 = 39 nM) and increases mitochondrial motility in neurons expressing ApoE4 (EC50 = <1 nM)

Formal name: 4-[[4-[[2-(3,4-dihydro-3-methyl-4-oxo-1-phthalazinyl)acetyl]amino]phenyl]methyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester

Synonyms: 

Molecular weight: 491.6

CAS: 1311174-68-1

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease

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