565790

Compound E

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

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₂₇H₂₄F₂N₄O₃
• Número CAS: 209986-17-4
• Peso molecular: 490.50
• Número MDL: MFCD04974531
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nome do produto: 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
• Ensaio: ≥95% (HPLC)
• Formulário: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: DMSO: 10 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: Fc1cc(cc(c1)CC(=O)N[C@@H](C)C(=O)NC2N=C(c4c(cccc4)N(C2=O)C)c3ccccc3)F
• 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
• chave InChI: JNGZXGGOCLZBFB-YPHZTSLFSA-N

Descrição

Descrição geral

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 p75^NTR. Only weakly affects presenilinase activity at much higher concentrations (200-400 µM).

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

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

Outras notas

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.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable