Gamma Secretase Inhibitor XXI, Compound E

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Gamma Secretase Inhibitor XXI, Compound E

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货号：565790-500UG

品牌：Millipore 密理博

配送至：

北京朝阳

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数量：

EA (预计3-5工作日到货)

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Replacement Information

重要规格表

Empirical Formula	CAS #
C₂₇H₂₄F₂N₄O₃	209986-17-4

Description
Overview	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).
Catalogue Number	565790
Brand Family	Calbiochem®
Synonyms	(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

References
References	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. Oncogene 22, 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. Science 294, 2179. Beher, D., et al. 2001. J. Biol. Chem. 276, 45394. Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312. Seiffert, D., et al. 2000. J. Biol. Chem. 275, 34086.

References

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. Oncogene 22, 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. Science 294, 2179.
Beher, D., et al. 2001. J. Biol. Chem. 276, 45394.
Doerfler, P., et al. 2001. Proc. Natl. Acad. Sci. USA 98, 9312.
Seiffert, D., et al. 2000. J. Biol. Chem. 275, 34086.

Product Information
CAS number	209986-17-4
ATP Competitive	N
Form	White solid
Hill Formula	C₂₇H₂₄F₂N₄O₃
Chemical formula	C₂₇H₂₄F₂N₄O₃
Reversible	N
Structure formula Image

Applications

Biological Information
Primary Target	γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
Primary Target IC<sub>50</sub>	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
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.