FLI-06

novel inhibitor of Notch signaling CAS# 313967-18-9

FLI-06

Catalog No. BCC5110----Order now to get a substantial discount!

Product Name & Size Price Stock
FLI-06: 5mg $81 In Stock
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Quality Control of FLI-06

Number of papers citing our products

Chemical structure

FLI-06

3D structure

Chemical Properties of FLI-06

Cas No. 313967-18-9 SDF Download SDF
PubChem ID 3103157 Appearance Powder
Formula C25H30N2O5 M.Wt 438.52
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 20 mM in ethanol
Chemical Name cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,6,8-tetrahydroquinoline-3-carboxylate
SMILES CC1=C(C(C2=C(N1)CC(CC2=O)(C)C)C3=CC=C(C=C3)[N+](=O)[O-])C(=O)OC4CCCCC4
Standard InChIKey SWWVFYHSSOWZMF-UHFFFAOYSA-N
Standard InChI InChI=1S/C25H30N2O5/c1-15-21(24(29)32-18-7-5-4-6-8-18)22(16-9-11-17(12-10-16)27(30)31)23-19(26-15)13-25(2,3)14-20(23)28/h9-12,18,22,26H,4-8,13-14H2,1-3H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of FLI-06

DescriptionInhibitor of Notch signaling (EC50 = 2.3 μM). Disrupts Notch trafficking and processing. Reduces amyloid β secretion. Changes the maturation and abolishes shredding of APP. Inhibits ER exporting and converts tubular ER to sheets.

FLI-06 Dilution Calculator

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FLI-06 Molarity Calculator

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Preparing Stock Solutions of FLI-06

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2804 mL 11.402 mL 22.804 mL 45.608 mL 57.0099 mL
5 mM 0.4561 mL 2.2804 mL 4.5608 mL 9.1216 mL 11.402 mL
10 mM 0.228 mL 1.1402 mL 2.2804 mL 4.5608 mL 5.701 mL
50 mM 0.0456 mL 0.228 mL 0.4561 mL 0.9122 mL 1.1402 mL
100 mM 0.0228 mL 0.114 mL 0.228 mL 0.4561 mL 0.5701 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on FLI-06

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.

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References on FLI-06

Inhibition of cargo export at ER exit sites and the trans-Golgi network by the secretion inhibitor FLI-06.[Pubmed:27587840]

J Cell Sci. 2016 Oct 15;129(20):3868-3877.

Export out of the endoplasmic reticulum (ER) involves the Sar1 and COPII machinery acting at ER exit sites (ERES). Whether and how cargo proteins are recruited upstream of Sar1 and COPII is unclear. Two models are conceivable, a recruitment model where cargo is actively transported through a transport factor and handed over to the Sar1 and COPII machinery in ERES, and a capture model, where cargo freely diffuses into ERES where it is captured by the Sar1 and COPII machinery. Using the novel secretion inhibitor FLI-06, we show that recruitment of the cargo VSVG to ERES is an active process upstream of Sar1 and COPII. Applying FLI-06 before concentration of VSVG in ERES completely abolishes its recruitment. In contrast, applying FLI-06 after VSVG concentration in ERES does not lead to dispersal of the concentrated VSVG, arguing that it inhibits recruitment to ERES as opposed to capture in ERES. FLI-06 also inhibits export out of the trans-Golgi network (TGN), suggesting that similar mechanisms might orchestrate cargo selection and concentration at the ER and TGN. FLI-06 does not inhibit autophagosome biogenesis and the ER-peroxisomal transport route, suggesting that these rely on different mechanisms.

Small molecules intercept Notch signaling and the early secretory pathway.[Pubmed:24077179]

Nat Chem Biol. 2013 Nov;9(11):731-8.

Notch signaling has a pivotal role in numerous cell-fate decisions, and its aberrant activity leads to developmental disorders and cancer. To identify molecules that influence Notch signaling, we screened nearly 17,000 compounds using automated microscopy to monitor the trafficking and processing of a ligand-independent Notch-enhanced GFP (eGFP) reporter. Characterization of hits in vitro by biochemical and cellular assays and in vivo using zebrafish led to five validated compounds, four of which induced accumulation of the reporter at the plasma membrane by inhibiting gamma-secretase. One compound, the dihydropyridine FLI-06, disrupted the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A. FLI-06 inhibited general secretion at a step before exit from the endoplasmic reticulum (ER), which was accompanied by a tubule-to-sheet morphological transition of the ER, rendering FLI-06 the first small molecule acting at such an early stage in secretory traffic. These data highlight the power of phenotypic screening to enable investigations of central cellular signaling pathways.

Description

Inhibitor of Notch signaling,FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM.

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