FLI-06 --- Notch Pathway Modulator

FLI-06 is a novel potent and selective small molecule intercepting Notch signaling and the early secretory pathway (EC50 ~2.3 µM), identified by using automated microscopy to monitor the trafficking and processing of a ligand-independent Notch-GFP fusion reporter. FLI-06 can induce accumulation of the reporter at the plasma membrane by interfering with transport in the secretory pathway. It can also disrupt 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. FLI-06 is a very useful chemical probe to study the inhibition of membrane traffic at pre- ER-exit site (ERES) stages without fusion of ER-Golgi.

Product information

CAS Number: 313967-18-9

Molecular Weight: 438.52

Formula: C25H30N2O5

Chemical Name: cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate

Smiles: CC1NC2CC(C)(C)CC(=O)C=2C(C=1C(=O)OC1CCCCC1)C1C=CC(=CC=1)[N+]([O-])=O

InChiKey: SWWVFYHSSOWZMF-UHFFFAOYSA-N

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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

FLI-06 was used at 10 µM final concentration in vitro and in cellular assays.

In Vivo:

FLI-06 was applied at 50 μM in E3 embryo medium to zebrafish embryos with chorions torn but not completely removed from the sphere stage until the stage of analysis.

References:

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

Products are for research use only. Not for human use.

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