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Compound E {[allProObj[0].p_purity_real_show]}

货号:A1145654 同义名: γ-Secretase-IN-1; γ-Secretase Inhibitor XXI

Compound E是 γ-secretase 的抑制剂,抑制 γ-分泌酶介导的 Notch 裂解,IC50 值为 0.32 nM。Compound E还可抑制促性腺激素依赖性卵泡生长并阻止发育进入排卵前阶段。Compound E抑制神经母细胞瘤细胞的生长、分化和运动能力,加速人类胚胎干细胞向原始神经干细胞的分化。

Compound E 化学结构 CAS号:209986-17-4
Compound E 化学结构
CAS号:209986-17-4
Compound E 3D分子结构
CAS号:209986-17-4
Compound E 化学结构 CAS号:209986-17-4
Compound E 3D分子结构 CAS号:209986-17-4
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Compound E 纯度/质量文件 产品仅供科研

货号:A1145654 标准纯度: {[allProObj[0].p_purity_real_show]}
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Compound E 生物活性

描述 Compound E inhibits the growth of T47D and MCF-7 cell lines by less than 50% at a 50 μM concentration[1].
体外研究

Compound E inhibits the growth of T47D and MCF-7 cell lines by less than 50% at a 50 μM concentration[1].

Compound E 细胞实验

Cell Line
Concentration Treated Time Description References
MT-1 cells 5μM 24 h Compound E induced caspase-9 and caspase-3 activities. Leukemia. 2015 Mar;29(3):556-66
MT-1 cells 10μM 48 h Compound E induced apoptosis in MT-1 cells. Leukemia. 2015 Mar;29(3):556-66
IMR-32 neuroblastoma cells 10 μM 5 days To evaluate the effects of GSIs alone or in combination with 13-cis retinoic acid (RA) on neuroblastoma cell growth, differentiation, and migration. Results showed that GSIs alone induced complete cell growth arrest, promoted neuronal differentiation, and significantly reduced cell motility. The combination with 13-cis RA enhanced these effects. Neuro Oncol. 2010 Dec;12(12):1231-43
SH-SY5Y neuroblastoma cells 10 μM 5 days To evaluate the effects of GSIs alone or in combination with 13-cis retinoic acid (RA) on neuroblastoma cell growth, differentiation, and migration. Results showed that GSIs alone induced complete cell growth arrest, promoted neuronal differentiation, and significantly reduced cell motility. The combination with 13-cis RA enhanced these effects. Neuro Oncol. 2010 Dec;12(12):1231-43
MT-1 cells 0, 0.1, 0.5, 1.25, 2.5, 5 or 10μM 48 h Compound E suppressed MT-1 cell proliferation in a dose-dependent manner. Leukemia. 2015 Mar;29(3):556-66
HK-2 cells 100 nM 72 h To evaluate the effects of Compound E on TGF-β1 and fibronectin secretion in HK-2 cells. Results showed that Compound E alone significantly increased TGF-β1 and fibronectin secretion, similar to the effects of high albumin concentrations. Br J Pharmacol. 2013 Jul;169(6):1239-51
Bovine polymorphonuclear neutrophils (PMN) 20 nM 30 min Inhibition of Notch signaling to assess its effect on C. parvum-induced NETosis. Results showed that Compound E significantly reduced NET formation. Biology (Basel). 2022 Mar 14;11(3):442
bovine monocytes 20 nM 30 min Inhibition of Notch signaling pathway, reducing C. parvum-induced METosis Biology (Basel). 2023 Jul 5;12(7):961

Compound E 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
NOG mice MT-1 adult T-cell leukemia model Subcutaneous osmotic pump 10μmol/Kg Continuous administration for 28 days Compound E alone or in combination with Bortezomib and Romidepsin significantly inhibited tumor growth and prolonged the survival of leukemia-bearing mice. Leukemia. 2015 Mar;29(3):556-66

Compound E 动物研究

Dose Guinea-pig: 3 mg/kg - 30 mg/kg[1] (p.o.)
Administration p.o.

Compound E 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.

Compound E 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.19mL

2.04mL

1.02mL

20.39mL

4.08mL

2.04mL

Compound E 技术信息

CAS号209986-17-4
分子式C27H24F2N4O3
分子量 490.5
SMILES Code O=C(N[C@@H](C)C(N[C@@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)=O)CC4=CC(F)=CC(F)=C4
MDL No. MFCD04974531
别名 γ-Secretase-IN-1; γ-Secretase Inhibitor XXI; GSI-XXI
运输蓝冰
InChI Key JNGZXGGOCLZBFB-IVCQMTBJSA-N
Pubchem ID 11306390
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 105 mg/mL(214.07 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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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