| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Golgicide A (GCA), a quinoline compound, is a cell-permeable, potent and rapidly reversible inhibitor of GBF1, which is one of the guanine nucleotide exchange factors (ArfGEFs). It is also an inhibitor of shiga toxin cytotoxicity. 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.
| Targets |
GBF1
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|---|---|---|---|
| ln Vitro |
Golgicide A inhibits the effect of shiga toxin on protein synthesis with an IC50 of 3.3 μM. Golgicide A causes a decrease in GBF1-mediated Arf1 activation, arrests secretion of soluble and membrane-anchored proteins and then impairs retrograde toxin transport. Golgicide A decreases HCV RNA levels in FLRP1 cells and J6/JFH1 cells. In addition, Golgicide A causes redistribution of NS5A and accumulation of infectious viral particles in J6/JFH1 cells.
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| ln Vivo |
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| Cell Assay |
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. 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.
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| Animal Protocol |
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| References | |||
| Additional Infomation |
Golgicide A is a diastereoisomeric mixture comprising racemic cis- and racemic trans-goglioside A in a 10:1 ratio. It is a potent and rapidly reversible GBF1 (Golgi-specific brefeldin A-resistance guanine nucleotide exchange factor 1) inhibitor. The (3aS,4R,9bR) isomer is the most active (see Bioorg. Med. Chem. Lett., 2012, 22, 5177-5181). It has a role as a cis-Golgi ArfGEF GBF inhibitor. It contains a cis-golgicide A and a trans-golgicide A.
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| Molecular Formula |
C17H14F2N2
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| Molecular Weight |
284.310
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| Exact Mass |
284.113
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| Elemental Analysis |
C, 71.82; H, 4.96; F, 13.36; N, 9.85
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| CAS # |
1139889-93-2
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| Related CAS # |
Golgicide A-2;1394285-50-7;Golgicide A-1;1394285-49-4;(Rac)-Golgicide A;1005036-73-6
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| PubChem CID |
25113626
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| Appearance |
White to off-white solid powder
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| LogP |
4.324
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
414
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1C=CC2C1C(NC3=C2C=C(C=C3F)F)C4=CN=CC=C4
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| InChi Key |
NJZHEQOUHLZCOX-FTLRAWMYSA-N
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| InChi Code |
InChI=1S/C17H14F2N2/c18-11-7-14-12-4-1-5-13(12)16(10-3-2-6-20-9-10)21-17(14)15(19)8-11/h1-4,6-9,12-13,16,21H,5H2/t12-,13+,16?/m0/s1
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| Chemical Name |
(3aR,9bS)-6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 57~100 mg/mL ( 200.49~351.74 mM )
Ethanol : 4 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 3: 10% DMSO+90% (20% SBE-β-CD in Saline): ≥ 2.5 mg/mL (8.79 mM) (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5173 mL | 17.5864 mL | 35.1729 mL | |
| 5 mM | 0.7035 mL | 3.5173 mL | 7.0346 mL | |
| 10 mM | 0.3517 mL | 1.7586 mL | 3.5173 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06244069 | Not yet recruiting | Diagnostic Test: Temporal arterial biopsy Diagnostic Test: Whole exome sequencing |
Giant Cell Arteritis Temporal Arteritis |
ASST Fatebenefratelli Sacco | March 2024 | |
| NCT06271018 | Not yet recruiting | Giant Cell Arteritis Aortitis |
GMIOFrance | April 1, 2024 | ||
| NCT05749094 | Not yet recruiting | Diagnostic Test: Optic nerve ultrasound | Giant Cell Arteritis Anterior Ischemic Optic Neuropathy |
Hopital du Sacre-Coeur de Montreal | March 2024 | |
| NCT03725202 | Active, not recruiting | Drug: Upadacitinib Drug: Corticosteroid (CS) |
Giant Cell Arteritis (GCA) | AbbVie | January 24, 2019 | Phase 3 |
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