FLI-06, disrupted the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A. FLI-06 inhibited general secretion at a step before exit from the endoplasmic reticulum. In FLI-06–treated cells, no APPCTF accumulates despite strongly reduced Aβ secretion, suggesting that it acts upstream of α-secretase and β-secretase cleavage. FLI-06 is a very useful chemical probe to study the inhibition of membrane traffic at pre- ER-exit site (ERES) stages without fusion of ER-Golgi[1].
Kinase Assay
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].
Cell Assay
Animal Administration
References
[1]. Kramer A, et al. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol. 2013 Nov;9(11):731-8.
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