Description | γ-Secretase-IN-1 is a potent γ-secretase inhibitor that displays partial antiproliferative activity on T-47D cells and inhibits β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage. |
In vitro | At a concentration of 50 μM, compound E reduces the proliferation of T47D and MCF-7 cell lines by less than 50% [2]. |
Target activity | β-amyloid(42):0.37 nM, Notch:0.24 nM, β-amyloid(40):0.24 nM |
Synonyms | Compound E |
molecular weight | 490.5 |
Molecular formula | C27H24F2N4O3 |
CAS | 209986-17-4 |
Storage | keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 80 mg/mL (163.10 mM), Sonication is recommended. |
References | 1. Rasul S, et al. Inhibition of gamma-secretase induces G2/M arrest and triggers apoptosis in breast cancer cells. Br J Cancer. 2009 Jun 16;100(12):1879-88. 2. Beher D, et al. Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology. J Biol Chem. 2001 Nov 30;276(48):45394-402. |