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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
FLI-06 (FLI 06; FLI-06) is a novel and potent inhibitor of Notch signaling pathway with EC50 of 2.3 μM. Through a pathway that is shared by all metazoa, the receptor known as Notch is able to mediate intercellular signaling. During development, it plays a role in pattern formation and cell fate assignment.
| Targets |
Notch (EC50 = 2.3 μM)
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|---|---|
| ln Vitro |
FLI-06 prevents Notch trafficking and processing in HeLa NotchΔE-eGFP cells. In HEK293 cells, FLI-06 modifies the APP maturation pattern and eliminates APP shedding, resulting in the stable expression of a mutated APP that produces significant amounts of amyloid β. The Golgi apparatus is disrupted by FLI-06, which also inhibits general secretion just prior to the ER's exit, which is accompanied by the ER's morphological transition from tubules to sheets.[1]
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| ln Vivo |
FLI-06 (50 μM) inhibits zebrafish embryos' natural Notch signaling.[1]
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| Enzyme Assay |
The test compounds' EC50 values are determined using a serial dilution series with concentrations ranging from 200 to 0.1 μM. 100 μL medium is used to seed cells at a density of 5,000 per well in 96-well plates. The following day, 100 μL of each test compound's medium is added. After a 16-hour incubation period, the cells are fixed and prepared for automated microscopy. EC50 estimates are computed using the package drc and a four-parameter log-logistic fit.
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| Cell Assay |
NotchΔE-eGFP accumulated and NICD-eGFP production decreased in HeLa NotchΔE-eGFP cells treated with FLI-06. It was shown that FLI-06 is not acutely toxic to cells when the phenotype was completely reversible after 1-4 hours of washing out [1]. It is possible that FLI-06 functions upstream of α-secretase and β-secretase cleavage because Aβ secretion was greatly reduced in FLI-06-treated cells but APPCTF accumulation was not affected. The Golgi was completely disrupted by FLI-06, according to immunofluorescence analysis of HeLa cells. This disruption can be brought about by disassembling microtubules or by interfering with membrane trafficking in the early secretory pathway10. Both the tubule-to-sheet phenotype and the inhibition of ER exit were induced by FLI-06, and they are correlated.
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| Animal Protocol |
Zebrafish embryos.
50 μM |
| References |
| Molecular Formula |
C25H30N2O5
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|---|---|---|
| Molecular Weight |
438.52
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| Exact Mass |
438.215
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| Elemental Analysis |
C, 68.47; H, 6.90; N, 6.39; O, 18.24
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| CAS # |
313967-18-9
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| Related CAS # |
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| PubChem CID |
3103157
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| Appearance |
white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
597.5±50.0 °C at 760 mmHg
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| Flash Point |
315.2±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.596
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| LogP |
4.47
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
852
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C([N+]([O-])=O)C=C3)OC4CCCCC4
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| InChi Key |
SWWVFYHSSOWZMF-UHFFFAOYSA-N
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| InChi Code |
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
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| Chemical Name |
cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,6,8-tetrahydroquinoline-3-carboxylate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.70 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2804 mL | 11.4020 mL | 22.8040 mL | |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5608 mL | |
| 10 mM | 0.2280 mL | 1.1402 mL | 2.2804 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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