Identification and Preclinical Pharmacology of the -Secretase Modulator BMS-869780
BMS-869780 did not inhibit Notch cleavage in vitro. (a) HeLa cell cultures were transfected with mNotchE and CBF1-luciferase reporter constructs, treated overnight with BMS-869780 (●), BMS-299897 (▲), or BMS-433796 (■), and luciferase assays were carried out. (b) HeLa cell cultures were transfected with mNotch1865, treated with compounds overnight, and cell extracts were evaluated by western blot using anti-c-myc-HRP conjugate. Lanes 1 and 9: DMSO (0.1%) vehicle. Lane 2: BMS-299897 at 1 μM. Lane 3: BMS-433796 at 0.3 μM. Lanes 4–8: BMS-869780 at 0.1, 0.3, 1, 3, and 10 μM, respectively.
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