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Gamma Secretase

FLI-06 (313967-18-9)

FLI-06 is a novel inhibitor of Notch signaling with EC50 of 2.3 μM. FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A.

Not Intended for Therapeutic Use. For research use only.

CAS: 313967-18-9 Category

FLI-06 (313967-18-9) Description:

FLI-06 is a Notch inhibitor and the early secretory pathway inhibitor. FLI-06 disrupts the Golgi apparatus in a manner distinct from that of brefeldin A and golgicide A. FLI-06 inhibits 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. FLI-06 is the first small molecule acting at such an early stage in secretory traffic. Notch signaling has a pivotal role in numerous cell-fate decisions, and its aberrant activity leads to developmental disorders and cancer.

FLI-06 (313967-18-9) Specifications:

Product Name FLI-06
Synonyms FLI06; FLI 06; FLI06.
Chemical Names cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate
Purity >98% (or refer to the Certificate of Analysis)
CAS Number 313967-18-9
Molecular Formula C25H30N2O5
Molecular Weight 438.5161
Monoisotopic Mass 438.215 g/mol
MDL number N/A
InChIKey SWWVFYHSSOWZMF-UHFFFAOYSA-N
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
SMILES O=C(C1=C(C)NC2=C(C(CC(C)(C)C2)=O)C1C3=CC=C([N+]([O-])=O)C=C3)OC4CCCCC4
Form Powder
Color white to beige
Solubility  Soluble in DMSO, not in water
Storage Temp.  Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Shelf life >2 years if stored properly
Handling Protect from air and light
Application FLI-06 is an inhibitor of Notch signaling with an EC50 of 2.3 μM.

 


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RIDADR NONH for all modes of transport

References:

  • 1: Krämer A, Mentrup T, Kleizen B, Rivera-Milla E, Reichenbach D, Enzensperger C, Nohl R, Täuscher E, Görls H, Ploubidou A, Englert C, Werz O, Arndt HD, Kaether C. Small molecules intercept Notch signaling and the early secretory pathway. Nat Chem Biol. 2013 Nov;9(11):731-8. doi: 10.1038/nchembio.1356. Epub 2013 Sep 29. PubMed PMID: 24077179.
  • 2: FLI-06 suppresses proliferation, induces apoptosis and cell cycle arrest by targeting LSD1 and Notch pathway in esophageal squamous cell carcinoma cells. Lu Z, Ren Y, Zhang M, Fan T, Wang Y, Zhao Q, Liu HM, Zhao W, Hou G. Biomed Pharmacother. 2018 Nov;107:1370-1376. doi: 10.1016/j.biopha.2018.08.140. Epub 2018 Aug 31.
  • 3: Inhibition of cargo export at ER exit sites and the trans-Golgi network by the secretion inhibitor FLI-06. Yonemura Y, Li X, Müller K, Krämer A, Atigbire P, Mentrup T, Feuerhake T, Kroll T, Shomron O, Nohl R, Arndt HD, Hoischen C, Hemmerich P, Hirschberg K, Kaether C. J Cell Sci. 2016 Oct 15;129(20):3868-3877. Epub 2016 Sep 1.
  • 4: The Dengue Virus Nonstructural Protein 1 (NS1) Is Secreted from Mosquito Cells in Association with the Intracellular Cholesterol Transporter Chaperone Caveolin Complex. Rosales Ramirez R, Ludert JE. J Virol. 2019 Feb 5;93(4). pii: e01985-18. doi: 10.1128/JVI.01985-18. Print 2019 Feb 15.
  • 5: Notch signaling pathway regulates cell cycle in proliferating hepatocytes involved in liver regeneration. Zhang F, Zhang J, Li X, Li B, Tao K, Yue S. J Gastroenterol Hepatol. 2018 Aug;33(8):1538-1547. doi: 10.1111/jgh.14110. Epub 2018 Mar 24.