Potent γ-secretase inhibitor (GSI; IC50 value 4 nM) targeting Notch signaling with in vivo efficacy in various tumor cells, showing >100-fold selectivity with respect to 75 other proteins of various types (receptors, ion channels, and enzymes). Treatment of HEK293 cells with RO4929097 caused a dose-dependent decrease in the amount of Aβ peptides secreted into the culture medium (EC50 value 14 nM), and a strong dose-dependent inhibition of Notch processing in a Notch cell-based reporter assay (EC50 value 5 nM).

KEYWORDS: RO 4929097 | Supplier | γ-Secretase inhibitor | RO4929097 | CAS [847925-91-1] | Amyloids | γ Secretase | Inhibitor | GSI | Notch | signaling | Aβ peptides | tumor | melanoma | gamma Secretase