5.09230

ER Export Inhibitor II, FLI-06

• Synonym(s): ER Export Inhibitor II, FLI-06, Cyclohexyl 2,7,7-trimethyl-4-(4-nitrophenyl)-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate, Cyclohexyl 4-(4ʹ-nitrophenyl)-2,7,7-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate, FLI06
• Empirical Formula (Hill Notation): C₂₅H₃₀N₂O₅
• Molecular Weight: 438.52
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Assay: ≥95% (HPLC)
• Quality Level: 100
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: yellow
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Description

General description

A cell-permeable, non-toxic, dihydropyridine compound that prevents cellular maturation/glycosylation and surface expression of Notch, APP, Klotho (Effect. conc. = 10 µM in HEK293, HeLa, U2OS cultures) in a rapid and reversible manner by blocking events prior to cargo assembly at the endoplasmic reticulum exit sites (ERES) without affecting cytoskeleton, endocytosis, or other post-ERES events targeted by BFA, GCA, Exo1, A5, Retro-2, U18666A, or Vacuolin-1 (Cat. nos. 203729, 345862, 341220, 444805, 554715, 662015, & 673000, respectively). Notch signaling is shown to be effectively inhibited by treatment with either FLI-06 or the γ-Secretase inhibitior DAPT (Cat. nos. 565770 & 565784) in both C2C12 cultures (10 µM FLI-06) in vitro and in zebrafish embryos (50 µM FLI-06) in vivo.

A cell-permeable, non-toxic, dihydropyrimidine compound that prevents cellular glycosylation and surface expression of Notch, APP, Klotho (Effect. conc. = 10 µM in HEK293, HeLa, U2OS cultures) in a rapid and reversible manner by blocking events prior to cargo assembly at the ER exit sites (ERES) without affecting other post-ERES events targeted by BFA, GCA, Exo1, A5, Retro-2, U18666A, or Vacuolin-1 (Cat. nos. 203729, 345862, 341220, 444805, 554715, 662015, & 673000, respectively). Notch signaling is shown to be effectively inhibited by treatment with either FLI-06 or the γ-Secretase inhibitior DAPT (Cat. nos. 565770 & 565784) in both C2C12 cultures (10 µM FLI-06) in vitro and in zebrafish embryos (50 µM FLI-06) in vivo.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ER

Reversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°). Stock solutions are stable for up to 6 months at -20°C.

Use only fresh DMSO for reconstitution.

Other Notes

Kramer, A., et al. 2013. Nat. Chem. Biol.9, 731.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable