PH-002

Catalog No.S0082 Batch:S008201

Technical Data

Formula	C₂₇H₃₃N₅O₄
Molecular Weight	491.58	CAS No.	1311174-68-1
Solubility (25°C)*	In vitro	DMSO	98 mg/mL (199.35 mM)
		Ethanol	25 mg/mL (50.85 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description	PH-002 is an inhibitor of Apolipoprotein E4 (ApoE4) intracellular domain interaction in nerve cells.
In vitro	PH-002 is the small-molecule structure corrector for apolipoprotein (apo) E4, which can disrupt domain interaction in Neuro-2a cells and rescue the impaired intracellular trafficking of apoE4.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Wild type Neuro-2a neuroblastoma cells Concentrations 100 nM Incubation Time 72 h Method Neuro-2a cells are transfected withEGFP-apoE3, EGFP-apoE4, and EGFP-apoE4-R61T using Lipofectamine 2000 and selected with 400 μg/ml neomycin for 4 weeks. Colonies with green fluorescence are picked for further enrichment. Neuro-2a cells are seeded at 7500-8000 cells/well on 24-well plates containing Opti-MEM with DMSO plus 100 nM PH002 for 72 h. Cells are plated 2 days before the FRAP measurement experiment in eight-well chamber slides with a coverglass bottom coated with PL-lysine at 5000 cells/well. Recordings are obtained with an inverted Leica SP5 confocal microscope and a 63×oil objective with a numerical aperture of 1.4; cells are maintained at 37 ℃ in 5% CO₂.

Cell Assay:^{^[1]}

Cell lines
Wild type Neuro-2a neuroblastoma cells
Concentrations
100 nM
Incubation Time
72 h
Method
Neuro-2a cells are transfected withEGFP-apoE3, EGFP-apoE4, and EGFP-apoE4-R61T using Lipofectamine 2000 and selected with 400 μg/ml neomycin for 4 weeks. Colonies with green fluorescence are picked for further enrichment. Neuro-2a cells are seeded at 7500-8000 cells/well on 24-well plates containing Opti-MEM with DMSO plus 100 nM PH002 for 72 h. Cells are plated 2 days before the FRAP measurement experiment in eight-well chamber slides with a coverglass bottom coated with PL-lysine at 5000 cells/well. Recordings are obtained with an inverted Leica SP5 confocal microscope and a 63×oil objective with a numerical aperture of 1.4; cells are maintained at 37 ℃ in 5% CO₂.

References

[1] Brodbeck J, et al. J Biol Chem. 2011 May 13;286(19):17217-26.

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SHIPPING AND STORAGE
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