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Compound E

An inhibitor of γ-secretase

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Compound E的二维码
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  • 货号: ajce50478
  • CAS: 209986-17-4
  • 别名: N-[(1S)-2-[[(3S)-2,3-二氢-1-甲基-2-氧代-5-苯基-1H-1,4-苯并二氮杂卓-3-基]氨基]-1-甲基-2-氧代乙基]-3,5-二氟苯乙酰胺,γ-Secretase-IN-1
  • 分子式: C27H24F2N4O3
  • 分子量: 490.5
  • 纯度: >98%
  • 溶解度: DMSO: 100 mg/mL (203.87 mM)
  • 储存: Store at -20°C, sealed storage, away from moisture and light
  • 库存: 现货

Background

γ-Secretase is a multimeric aspartyl protease that regulates signaling pathways by proteolytically cleaving substrates, abrogating or releasing signaling molecules.1 Two well-known substrates are the carboxyl-terminal fragments (CTFs) of the receptor Notch, which has key roles in development, and that of amyloid precursor protein (APP), which is important in Alzheimer’s disease.1 Compound E is a potent, cell-permeable, and selective inhibitor of γ-secretase, blocking the cleavage of both APP and Notch CTFs with IC50 values of ~0.3 nM.2,3,4 Compound E induces neuronal differentiation, impairs ovarian folliculogenesis, and suppresses thymocyte development by preventing Notch activation by γ-secretase.5,6,7


1.Jurisch-Yaksi, N., Sannerud, R., and Annaert, W.A fast growing spectrum of biological functions of γ-secretase in development and diseaseBiochim. Biophys. Acta1828(12)2815-2827(2013) 2.Seiffert, D., Bradley, J.D., Rominger, C.M., et al.Presenilin-1 and -2 are molecular targets for γ-secretase inhibitorsJ. Biol. Chem.275(44)34086-34091(2000) 3.Beher, D., Wrigley, J.D.J., Nadin, A., et al.Pharmacological knock-down of the presenilin 1 heterodimer by a novel g -secretase inhibitor. Implications for presenilin biologyJ. Biol. Chem.276(48)45394-45402(2001) 4.Zhao, G., Mao, G., Tan, J., et al.Identification of a new presenilin-dependent ζ-cleavage site within the transmembrane domain of amyloid precursor proteinJ. Biol. Chem.279(49)50647-50650(2004) 5.Ferrari-Toninelli, G., Bonini, S.A., Uberti, D., et al.Targeting Notch pathway induces growth inhibition and differentiation of neuroblastoma cellsNeuro. Oncol.12(12)1231-1243(2010) 6.Jovanovic, V.P., Sauer, C.M., Shawber, C.J., et al.Intraovarian regulation of gonadotropin-dependent folliculogenesis depends on notch receptor signaling pathways not involving Delta-like ligand 4 (Dll4)Reprod. Biol. Endocrinol.1143(2013) 7.Doerfler, P., Shearman, M.S., and Perlmutter, R.M.Presenilin-dependent γ-secretase activity modulates thymocyte developmentProc. Natl. Acad. Sci. USA98(16)9312-9317(2001)

Protocol

Cell experiment:

The breast cancer cell lines MDA-MB-231, T47D, and MCF-7 are treated with Compound E at concentrations in the range 0.01-50?μM for 48?h and their viability is determined using a Coulter counter[1].

参考文献:

[1]. Beher D, et al. Pharmacological knock-down of the presenilin 1 heterodimer by a novel gamma -secretase inhibitor: implications for presenilin biology. J Biol Chem. 2001 Nov 30;276(48):45394-402.
[2]. Rasul S, et al. Inhibition of gamma-secretase induces G2/M arrest and triggers apoptosis in breast cancer cells. Br J Cancer. 2009 Jun 16;100(12):1879-88.

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