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].
体内研究
When administered chronically at a dosage of 10 mg/kg to TgCRND8 mice, LY-411,575 significantly reduces levels of brain and plasma Aβ40 and -42[1].
LY411575 lowers cortical Aβ40 in young transgenic CRND8 mice with an ED50 of approximately 0.6 mg/kg and causes significant thymus atrophy and intestinal goblet cell hyperplasia at doses exceeding 3 mg/kg. The severity of intestinal goblet cell hyperplasia induced by a 10 mg/kg dose of LY411575 is consistent across both young and aged mice[3].
Additionally, LY411575 has been shown to inhibit the formation of proliferative vitreoretinopathy (PVR) in mice, demonstrating its effectiveness in vivo[5].
体外研究
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].
LY-411575 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
CHO cells
Function assay
24 h
Reduction of human wild type PS1-induced amyloid beta-42 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000135 μM
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
CHO cells
Function assay
24 h
Reduction of human wild type PS1-induced amyloid beta-42 level in CHO cells overexpressing human APP751 after 24 hrs by liquid phase electrochemiluminescence assay relative to control, EC50=0.000135 μM
17573346
H4 cells
100 nM
Function assay
16 h
Inhibition of gamma secretase expressed in human H4 cells expressing BRI-C99 fusion protein assessed as C99 fragment accumulation fragment at 100 nM incubated for 16 hrs in by immunoblot
23181502
H4 cells
100 nM
Function assay
16 h
Inhibition of gamma secretase expressed in human H4 cells assessed as reduction in C83 levels at 10 uM incubated for 16 hrs by immunoblot
23181502
H4 cells
10 uM
Function assay
16 h
Inhibition of gamma secretase expressed in human H4 cells assessed as reduction in CTF levels at 10 uM incubated for 16 hrs by immunoblot
23181502
HEK293 cells
Function assay
Inhibition of gamma secretase in human HEK293 cells assessed as amyloid beta 40 production, EC50=0.000119 μM
17573346
HEK293 cells
Function assay
3 days
Modulation of gamma-secretase in HEK293 cells expressing guinea pig Swedish mutant SFV-APP695sw coexpressing DLL4 assessed as inhibition of notch processing in human TE671 cells after 3 days by dual-cell luciferase reporter gene assay, IC50=1.2 μM
24139583
SH-SY5Y cells
Function assay
Inhibition of gamma secretase-mediated amyloid beta (1 to 40) production in human SH-SY5Y cells, IC50=0.001 μM
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