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