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LY-411575

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Chemical Structure| 209984-57-6 同义名 : -
CAS号 : 209984-57-6
货号 : A140795
分子式 : C26H23F2N3O4
纯度 : 99%+
分子量 : 479.475
MDL号 : MFCD09832551
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+0.5% Tween80+5% propylene glycol+water 30 mg/mL suspension

生物活性
描述 LY-411,575 inhibits Notch activation, leading to apoptosis in both primary and immortalized KS cells. At a concentration of 500 μM, LY-411,575 causes G2/M growth arrest in SLK cells[2]. LY411575 effectively reduces the levels of intracellular HCV RNA with an IC50 of 0.56 ± 0.20 μM and also decreases extracellular HCV particles. When used alone or in combination with BMS-790052 at concentrations ranging from 0-40 nM, LY411575 lowers supernatant infectious titers in a dose-dependent manner, showing synergistic effects in reducing infectious virus production. Additionally, a 10 μM dose of LY411575 impairs ROS production in cells infected with HCVcc[4]. In vitro, LY411575 markedly reduces epithelial-mesenchymal transition (EMT) by inhibiting Notch signaling activation[5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay 24 h Reduction of human PS1 delta exon9 mutant-induced amyloid beta-42 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000352 μM 17573346
CHO cells Function assay 24 h Reduction of human PS1 delta exon9 mutant-induced amyloid beta-40 level in CHO cells overexpressing human APP751after 24 hrs by liquid phase electrochemiluminescence assay relative to control 17573346
CHO cells Function assay 24 h Reduction of human wild type PS1-induced amyloid beta-40 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000114 μM 17573346
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.43mL

2.09mL

1.04mL

20.86mL

4.17mL

2.09mL
参考文献

[1]Wong GT, et al. Chronic treatment with the gamma-secretase inhibitor LY-411,575 inhibits beta-amyloid peptide production and alters lymphopoiesis and intestinal cell differentiation. J Biol Chem. 2004 Mar 26;279(13):12876-82.

[2]Otoguro T, et al. Inhibitory effect of presenilin inhibitor LY411575 on maturation of hepatitis C virus core protein, production of the viral particle and expression of host proteins involved in pathogenicity. Microbiol Immunol. 2016 Nov;60(11):740-753

[3]Curry CL, et al. Gamma secretase inhibitor blocks Notch activation and induces apoptosis in Kaposi's sarcoma tumor cells. Oncogene. 2005 Sep 22;24(42):6333-44.

[4]Zhang J, et al. Notch signaling modulates proliferative vitreoretinopathy via regulating retinal pigment epithelial-to-mesenchymal transition. Histochem Cell Biol. 2017 Mar;147(3):367-375.

[5]Hyde LA, et al. Studies to investigate the in vivo therapeutic window of the gamma-secretase inhibitor N2-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl]-N1-[(7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl]-L-alaninamide (LY411,575) in the CRND8 mouse. J Pharmacol Exp Ther. 2006 Dec;319(3):1133-43.