209986-17-4

209986-17-4 structure

Name: Compound E
Chemical Name: γ-Secretase Inhibitor XXI
CAS Number: 209986-17-4
Molecular Formula: C₂₇H₂₄F₂N₄O₃
Molecular Weight: 490.501
Catalog: Signaling Pathways Neuronal Signaling γ-secretase
Create Date: 2017-01-22 08:36:00
Modify Date: 2024-01-07 23:05:41
Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.

Name	γ-Secretase Inhibitor XXI
Synonyms	COMPOUND E ((2S)-2-(AMINO)-N-PROPANAMIDE) Gamma-Secretase Inhibitor XXI Benzeneacetamide, N-[(1S)-2-[[(3S)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]amino]-1-methyl-2-oxoethyl]-3,5-difluoro- Compound E N-[(3,5-Difluorophenyl)acetyl]-N-[(3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl]-L-alaninamide

Description	Compound E is a γ-secretase inhibitor. Compound E bloks β-amyloid(40), β-amyloid(42), and Notch γ-secretase cleavage with IC50s of 0.24, 0.37, 0.32 nM, respectively.
Related Catalog	Signaling Pathways >> Neuronal Signaling >> γ-secretase Signaling Pathways >> Stem Cell/Wnt >> γ-secretase Research Areas >> Cancer
Target	IC50: 0.24 nM (β-amyloid(40)), 0.37 nM (β-amyloid(42)), 0.24 nM (Notch)[1]
In Vitro	Compound E reduces the proliferation of T47D, and MCF-7 cell lines by less than 50% at a concentration of 50 μM[1].
Cell Assay	The breast cancer cell lines MDA-MB-231, T47D, and MCF-7 are treated with Compound E at concentrations in the range 0.01-50 μM for 48 h and their viability is determined using a Coulter counter[1].
References	[1]. 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. [2]. 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.