PH-002, inhibitor

PH-002

Cat. Num. AAA5755369

• Purity: 98.00%
• Synonyms: PH-002; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 75mg/mL (152.57mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C27H33N5O4
• SMILES: O=C(N1CCN(CC2=CC=C(NC(CC3=NN(C)C(C4=C3C=CC=C4)=O)=O)C=C2)CC1)OC(C)(C)C
• CAS Number: 1311174-68-1
• Target & IC50: Apo E4 in FRET: ic50 116nM
• In Vitro: PH-002 (100nM) enhances 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). PH-002 is also shown to enhance COX1 levels in primary neurons from the NSE-apoE4 transgenic mouse cortex and hippocampus. COX1 levels are increased by ~60% after 4 days of treatment with PH-002 (200nM) [2].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for PH-002, inhibitor

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

References

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.
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.
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.
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.