FLI06 是一种 Notch 信号传导的抑制剂,EC50=2.3 μM。
产品描述
FLI-06 is a Notch signaling inhibitor (EC50: 2.3 μM).
体外活性
在斑马鱼胚胎中,FLI-06(50uM)可使内源性的Notch信号被抑制.
体内活性
在肾上皮细胞系293细胞中,稳定转染突变型的APP可产生大量的淀粉样沉淀。FLI-06可使APP的成熟模式改变,从而终止APPs的释放。在过表达Notch绿色荧光蛋白的Hela细胞中,FLI-06抑制Notch的转运和进程。FLI-06可破坏高尔基复合体,在内质网从管状转换到片状形态的过程中,使内质网转运前总蛋白的分泌受到抑制。
激酶实验
EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1].
Cas No.
313967-18-9
分子式
C25H30N2O5
分子量
438.524
别名
FLI 06
储存和溶解度
Ethanol:8.8 mg/mL (20 mM)
DMSO:43.9 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years