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Golgicide A (Synonyms: GCA)

Catalog No.GC16585

GBF1 inhibitor, potent, reversible and highly specific

Products are for research use only. Not for human use. We do not sell to patients.

Golgicide A Chemical Structure

Cas No.: 1139889-93-2, 1005036-73-6

Size Price Stock Qty
5mg
$59.00
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10mg
$104.00
In stock
25mg
$204.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

The human hepatoma cell line Huh7 (Huh7.5 cells were electroporated with the J6/JFH1 RNA and were transfected with an NS5A-encoding plasmid.)

Preparation method

The solubility of this compound in DMSO is >13mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10μM for 4, 24, and 48 h.

Applications

Treatment of cells with golgicide A, a drug that specifically inhibits GBF1, had been shown to decrease HCV (hepatitis C virus) RNA replication. Thus, golgicide A treatments diminished Arf1 (ADP-ribosylation factor 1) and HCV RNA levels in the JFH1-HCVcc cell system. In J6/JFH1 cells, some of the viral NS proteins migrated from speckle-like organelles to the peripheries of LDs in response to Arf1 inhibition by golgicide A treatment. Golgicide A treatments also decreased HCV RNA levels and cause redistribution of NS5A (a nonstructural protein) and accumulation of infectious viral particles.

References:

[1]. 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.

Background

ADP-ribosylation factor 1 (Arf1), when activated by guanine nucleotide exchange factors (ArfGEFs), plays a key role in regulating secretory traffic and membrane transport within the Golgi of eukaryotic cells. Golgicide A is a reversible inhibitor of the brefeldin A-resistant, cis-Golgi ArfGEF, GBF1 (IC50 = 3.3 µM).1 Inhibition of GBF1 via golgicide A can result in rapid dissociation of COPI vesicle coat protein from Golgi membranes and disassembly of the Golgi and trans-Golgi network.[1] Golgicide A does not affect the association of the adaptor protein, AP-1, or the Arf1-binding protein, GCA3, with the trans-Golgi network nor does it interfere with the activity of the ArfGEFs, BIG1 or 2.[1] Golgicide A can arrest the secretion of soluble and membrane-associated proteins at the ER-Golgi intermediate compartment, as well as prevent endocytic transport of Shiga toxin to the trans-Golgi network.[1]

Reference:
[1]. Saenz, J.B., Sun, W.J., Chang, J.W., et al. Golgicide A reveals essential roles for GBF1 in Golgi assembly and function. Nature Chemical Biology 5(3), 157-165 (2009).

Chemical Properties

Cas No. 1139889-93-2, 1005036-73-6 SDF
Synonyms GCA
Chemical Name (3aR,9bS)-6,8-difluoro-4-pyridin-3-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
Canonical SMILES C1C=CC2C1C(NC3=C(C=C(C=C23)F)F)C4=CN=CC=C4
Formula C17H14F2N2 M.Wt 284.3
Solubility 1mg/mL in ethanol, 10mg/mL in DMSO, 30mg/mL in DMF Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.5174 mL 17.5871 mL 35.1741 mL
5 mM 0.7035 mL 3.5174 mL 7.0348 mL
10 mM 0.3517 mL 1.7587 mL 3.5174 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 12 reference(s) in Google Scholar.)

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