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FLI-06 Sale

(Synonyms: 1,4,5,6,7,8-六氢-2,7,7-三甲基-4-(4-硝基苯基)-5-氧代-3-喹啉羧酸环己基酯) 目录号 : GC10211

A Notch inhibitor

FLI-06 Chemical Structure

Cas No.:313967-18-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,176.00
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10mg
¥987.00
现货
25mg
¥1,680.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

EC50 values of the test compounds are calculated from serial dilution series ranging from 200 to 0.1 μM. Cells are seeded in 96-well plates at a density of 5,000 cells per well in 100 μL medium. The next day, 100 μL medium containing each test compound is added. Cells are incubated for 16 h, fixed and processed for automated microscopy. EC50 estimates are calculated using four-parameter log-logistic fit with the package drc[1].

References:

[1]. Kramer A, et al. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol. 2013 Nov;9(11):731-8.

产品描述

FLI-06 is a novel inhibitor of Notch signaling with EC50 value of 2.3uM [1].
Notch signaling plays an important role in numerous cell-fate decisions, and its aberrant activity leads to cancer and developmental disorders [1].
Treatment of HeLa NotchΔE-eGFP cells with FLI-06 resulted in accumulation of NotchΔE-eGFP and reduced NICD-eGFP production. The phenotype was fully reversible within 1–4 h when washing out of FLI-06, which indicated that FLI-06 is not acutely toxic in cells [1]. In FLI-06 treated cells, Aβ secretion reduced significantly but not APPCTF accumulation, suggesting that FLI-06 acts upstream of α-secretase and β-secretase cleavage. Immunofluorescence analysis of HeLa cells revealed that FLI-06 caused a complete disruption of the Golgi, which can be caused by interfering with membrane trafficking in the early secretory pathway or by disassembly of the microtubules17. FLI-06 inhibited ER exit and also elicited the tubule-to-sheet phenotype, which are related to each other [1].
References:
[1]. Krämer A, Mentrup T, Kleizen B, et al. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol, 2013, 9(11): 731-738.

Chemical Properties

Cas No. 313967-18-9 SDF
别名 1,4,5,6,7,8-六氢-2,7,7-三甲基-4-(4-硝基苯基)-5-氧代-3-喹啉羧酸环己基酯
化学名 cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,6,8-tetrahydroquinoline-3-carboxylate
Canonical SMILES CC1=C(C(C2=C(N1)CC(CC2=O)(C)C)C3=CC=C(C=C3)[N+](=O)[O-])C(=O)OC4CCCCC4
分子式 C25H30N2O5 分子量 438.52
溶解度 ≥ 16.1mg/mL in DMSO 储存条件 Store at -20° C
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1 mg 5 mg 10 mg
1 mM 2.2804 mL 11.402 mL 22.804 mL
5 mM 0.4561 mL 2.2804 mL 4.5608 mL
10 mM 0.228 mL 1.1402 mL 2.2804 mL
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