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565790

Sigma-Aldrich

Compound E

≥95% (HPLC), solid, γ-secretase inhibitor, Calbiochem®

Synonim(y):

γ-Secretase Inhibitor XXI, Compound E, (S,S)- 2-[2-(3,5-Difluorophenyl)-acetylamino]-N-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-propionamide, Compound E

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About This Item

Wzór empiryczny (zapis Hilla):
C27H24F2N4O3
Numer CAS:
209986-17-4
Masa cząsteczkowa:
490.50
Kod UNSPSC:
12352200
NACRES:
NA.77

product name

γ-Secretase Inhibitor XXI, Compound E, This g-secretase inhibitor, CAS 209986-17-4, is a cell-permeable, potent, selective, non-transition-state analog inhibitor of γ-secretase and Notch processing. Lowers Aβ levels in APP transgenic mice

Próba

≥95% (HPLC)

Postać

solid

producent / nazwa handlowa

Calbiochem®

warunki przechowywania

OK to freeze
protect from light

kolor

white

rozpuszczalność

DMSO: 10 mg/mL

Warunki transportu

ambient

temp. przechowywania

2-8°C

InChI

1S/C27H24F2N4O3/c1-16(30-23(34)14-17-12-19(28)15-20(29)13-17)26(35)32-25-27(36)33(2)22-11-7-6-10-21(22)24(31-25)18-8-4-3-5-9-18/h3-13,15-16,25H,14H2,1-2H3,(H,30,34)(H,32,35)/t16-,25?/m0/s1

Klucz InChI

JNGZXGGOCLZBFB-YPHZTSLFSA-N

Opis ogólny

A cell-permeable, potent, selective, peptidomimetic, non-transition-state analog inhibitor of γ-secretase and Notch processing (IC50 = 300 pM for Aβ40 in CHO cells overexpressing wild type βAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40 and Aβ42 in SH-SY5Y cells stably transfected with SPA4CT). Lowers Aβ levels in several APP transgenic mouse models. Reported to bind to presenilins and suppress the proteolytic cleavage of transmembrane protein substrates, including APLP1 and APLP2, CD44, ErbB4, E-cadherin, low density lipoprotein receptor-related proteins, Notch ligands, and p75NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM).

Działania biochem./fizjol.

Cell permeable: yes
Primary Target
γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
Product does not compete with ATP.
Reversible: no
Target IC50: 300 pM for Aβ40 in CHO cells overexpressing wild typeβAPP; 240 pM for Aβ40, 370 pM for Aβ42, and 320 pM for NICD, respectively, in HEK293 cells stably transfected with βAPP695 and mNotchΔE(M1727V); 100 pM for both Aβ40

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Inne uwagi

Milano, J., et al. 2004. Toxicol. Sci.82, 341.
Jung, K.M., et al. 2003. J. Biol. Chem.278, 42161.
Murakami, D., et al. 2003. Oncogene22, 1511.
Campbell, W.A., et al. 2003. J. Neurochem.85, 1563.
Berechid, B.E., et al., 2002. J. Biol. Chem.277, 8154.
Lee, H.J., et al. 2002. J. Biol. Chem.277, 6318.
May, P., et al. 2002. J. Biol. Chem.277, 18736.
Scheinfeld, M.H., et al. 2002. J. Biol. Chem.277, 44195.
Ni, C. Y., et al. 2001. Science294, 2179.
Beher, D., et al. 2001. J. Biol. Chem.276, 45394.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA98, 9312.
Seiffert, D., et al. 2000. J. Biol. Chem.275, 34086.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
This page may contain text that has been machine translated.

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable

Certyfikaty analizy (CoA)

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