ER EXPORT INHIBITOR II FLI-06 (C15-1304-509)

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

Molecular Weight: 438.52. Empirical Formula: C₂₅H₃₀N₂O₅. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.