おすすめの製品
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
アッセイ
≥95% (HPLC)
形状
solid
メーカー／製品名
Calbiochem®
保管条件
OK to freeze
protect from light
色
white
溶解性
DMSO: 10 mg/mL
輸送温度
ambient
保管温度
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
InChI Key
JNGZXGGOCLZBFB-YPHZTSLFSA-N
詳細
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).
生物化学的／生理学的作用
Cell permeable: yes
Primary Target
γ-secretase and Notch processing Ab40 in CHO cells overexpressing wild type bAPP
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
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
再構成
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
その他情報
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.
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.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
この製品を見ている人はこちらもチェック
Kenichi Makino et al.
Journal for immunotherapy of cancer, 10(1) (2022-02-02)
Dendritic cells (DCs) play critical roles in regulating the innate and adaptive immune responses, and have long been a major focus of cancer immunotherapy. Accumulating evidence suggests that conventional type 1 DCs (cDC1s) excel in cross-presentation of exogenous antigens on
Claire E McGhee et al.
ACS central science, 7(11), 1809-1820 (2021-11-30)
Lithium has been a drug for bipolar disorders (BD) for over 70 years; however, its usage has been limited by its narrow therapeutic window (between 0.6 and 1.2 mM). Understanding the cellular distribution of lithium ions (Li+) in patient cells
Deli Hong et al.
Cancer research, 82(2), 248-263 (2021-11-24)
Neuroendocrine to nonneuroendocrine plasticity supports small cell lung cancer (SCLC) tumorigenesis and promotes immunogenicity. Approximately 20% to 25% of SCLCs harbor loss-of-function (LOF) NOTCH mutations. Previous studies demonstrated that NOTCH functions as a SCLC tumor suppressor, but can also drive
Nathaniel Safren et al.
The Journal of biological chemistry, 297(3), 101003-101003 (2021-07-26)
Autophagy is an evolutionarily conserved pathway mediating the breakdown of cellular proteins and organelles. Emphasizing its pivotal nature, autophagy dysfunction contributes to many diseases; nevertheless, development of effective autophagy modulating drugs is hampered by fundamental deficiencies in available methods for
Xiaoqing Zhu et al.
Science advances, 8(9), eabl7263-eabl7263 (2022-03-05)
Evolutionary mutations in primate-specific genes drove primate cortex expansion. However, whether conserved genes with previously unidentified functions also play a key role in primate brain expansion remains unknown. Here, we focus on BRN2 (POU3F2), a gene encoding a neural transcription
ライフサイエンス、有機合成、材料科学、クロマトグラフィー、分析など、あらゆる分野の研究に経験のあるメンバーがおります。.
製品に関するお問い合わせはこちら（テクニカルサービス）