| Description | PH-002, an inhibitor targeting the intramolecular domain interaction of apolipoprotein (apo) E4 in neuronal cells, additionally enhances mitochondrial motility and promotes neurite outgrowth, thereby countering related impairments. |
| In vitro | PH-002 是一种抑制神经细胞内apolipoprotein (apo) E4 分子内域相互作用的抑制剂，其半最大抑制浓度（IC50）为116 nM（FRET检测）[1]。 |
| In vivo | PH-002 (100 nM) 在NSE-apoE4基因转换小鼠来源的主要神经元中促进树突脊的发展，使其水平与NSE-apoE3主要神经元中的水平相当（使用PH-002处理的apoE3表达主要神经元与未经处理的主要神经元的结果相同）。PH-002还被证实能够在NSE-apoE4基因转换小鼠大脑皮层和海马体来源的主要神经元中提高COX1水平。经过4天的PH-002 (200 nM) 处理后，COX1水平增加了约60% [2]。 |
| Target activity | ApoE4 (FRET):116 nM |
| molecular weight | 491.58 |
| Molecular formula | C27H33N5O4 |
| CAS | 1311174-68-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 75 mg/mL (152.57 mM) |
| References | 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. |