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Compound E

Names

[ CAS No. ]:
209986-17-4

[ Name ]:
Compound E

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

DAPT (GSI-IX) | RO4929097 | YO-01027 | PF-3084014 | LY-411575 | L-685,458 | MK-0752 | Avagacestat | Semagacestat(LY450139) | Z-Ile-Leu-aldehyde | E 2012 | gamma-secretase modulator 1 | NGP555 | BMS 299897 | gamma-secretase modulator 3

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
778.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C27H24F2N4O3

[ Molecular Weight ]:
490.501

[ Flash Point ]:
424.7±32.9 °C

[ Exact Mass ]:
490.181641

[ PSA ]:
90.87000

[ LogP ]:
3.22

[ Vapour Pressure ]:
0.0±2.7 mmHg at 25°C

[ Index of Refraction ]:
1.624

[ Storage condition ]:
2-8℃

Related Compounds