Golgicide A
(Synonyms: GCA) 目录号 : GC16585
A reversible inhibitor of GBF1
Cas No.:1139889-93-2, 1005036-73-6
Sample solution is provided at 25 µL, 10mM.
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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).
| Cell experiment [1]: | |
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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.) |
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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. |
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Reacting condition |
10μM for 4, 24, and 48 h. |
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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. |
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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. |
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| Cas No. | 1139889-93-2, 1005036-73-6 | SDF | |
| 别名 | GCA | ||
| 化学名 | (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 | ||
| 分子式 | C17H14F2N2 | 分子量 | 284.3 |
| 溶解度 | 1mg/mL in ethanol, 10mg/mL in DMSO, 30mg/mL in DMF | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet