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565790 Sigma-Aldrichγ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem

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

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: (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

Primary Target: γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
209986-17-4	C₂₇H₂₄F₂N₄O₃

价格及供货情况

产品目录编号	库存情况	包装	数量 / 包装	价格	数量
565790-1MGCN	正在查询供货情况...... — 目前缺货有货停产少量现货供货情况有待确认登录查看库存有货目前缺货有货其余：另行通知其余：另行通知另行通知联系客户服务 Contact Customer Service 联系客户服务联系客户服务	玻璃瓶	1 mg	正在检索价格...... 无法检索价格。最小订购数量为倍数 Maximum Quantity is 以订单确认为准更多信息您节约了 ()。 — Request Pricing 登录查看价格	查看库存情况 —	添加到收藏夹添加到收藏夹添加到我的收藏夹
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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.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
565790-1MGCN	04055977191851
565790-500UGCN	04055977191868

Documentation

γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

γ-Secretase Inhibitor XXI, Compound E - CAS 209986-17-4 - Calbiochem 分析证书

标题	批号
565790	输入批号

参考

参考信息概述
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.

参考信息概述

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	04-April-2011 RFH
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
Description	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).
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	209986-17-4
Chemical formula	C₂₇H₂₄F₂N₄O₃
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (10 mg/ml)
Storage	Protect from light +2°C to +8°C
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.
Toxicity	Standard Handling
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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Neurobiology / Neurodegeneration > Secretase Inhibitors

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