Golgicide A

- Overview
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    Background
    
    Golgicide A is a potent, reversible and highly specific GBF1 inhibitor.GBF1, the ArfGEF responsible for Arf1 activation and COPI recruitment to cis-Golgi membranes, plays an important role in coordinating bidirectional transport and maintaining structural integrity of the Golgi [1].Golgicide A inhibits the effect of shiga toxin on protein synthesis with an IC50 of 3.3 μM in Vero cells. Immunofluoresence experiments demonstrates that Golgicide A causes complete dispersal of the medial-Golgi markers giantin and the cis-Golgi marker GM130 and results in a rapid redistribution of COPI from the Golgi. Also, Golgicide A causes a decrease in GBF1-mediated Arf1 activation, impairs retrograde toxin transport and arrests secretion of soluble and membrane-anchored proteins [1]. Golgicide A decreases HCV RNA levels and causes redistribution of NS5A in FLRP1 cells and J6/JFH1 cells. In addition, Golgicide A causes accumulation of infectious viral particles in J6/JFH1 cells [2].
    
    [1] Sáenz JB, Sun WJ, Chang JW, et al. Golgicide A reveals essential roles for GBF1 in Golgi assembly and function. Nat Chem Biol, 2009, 5(3): 157-165.
    [2] Matto M, Sklan EH, David N, et al. Role for ADP ribosylation factor 1 in the regulation of hepatitis C virus replication. J Virol, 2011, 85(2): 946-956.
- Properties
  - Alternative Name
    
    (3aS,9bR)-6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
    
    CAS Number
    
    1139889-93-2
    
    Molecular Formula
    
    C17H14F2N2
    
    Molecular Weight
    
    284.3
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥12.95 mg/mL in DMSO; ≥2.27 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Raphemot R, Toro-Moreno M, et al. "Discovery of Druggable Host Factors Critical to Plasmodium Liver-Stage Infection." Cell Chem Biol. 2019 Jun 12. pii: S2451-9456(19)30180-1. PMID:31257182

Golgicide A

Background

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