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|---|---|---|---|---|---|---|---|
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| 靶点 |
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| 描述 | Golgicide A serves as a powerful, highly selective, and reversible antagonist of GBF1, which is an ADP-ribosylation factor guanine nucleotide exchange factor (ArfGEF) associated with the cis-Golgi. It works as a strong and highly efficient inhibitor of shiga toxin's action. It effectively blocks the impact of shiga toxin on protein synthesis, exhibiting an IC50 value of 3.3 μM[1]. Golgicide A significantly inhibits the replication of coxsackievirus B3 (CVB3) as well as other types of human enteroviruses[2]. |
| Concentration | Treated Time | Description | References | |
| HeLa-ATCC cells | 20 μM | 5 h | Enhanced HAdV-C2-dE3B_GFP infection | J Virol. 2014 Nov;88(22):13086-98. |
| A549 cells | 20 μM | 5 h | Enhanced HAdV-C5-dE1_GFP infection | J Virol. 2014 Nov;88(22):13086-98. |
| primary astrocytes | 3.5 μM | 8 h | GCA reduced basal secreted Aβ levels | Cells. 2022 Aug 19;11(16):2585. |
| 293sw cells | 3.5 μM | 8 h | GCA reduced basal secreted Aβ levels | Cells. 2022 Aug 19;11(16):2585. |
| WI38 fibroblasts | 20 μM | 5 h | Not used | J Virol. 2014 Nov;88(22):13086-98. |
| M950822 and M980928 melanoma cells | 20 μM | 5 h | Enhanced HAdV-C5-dE1_GFP infection | J Virol. 2014 Nov;88(22):13086-98. |
| SF188 cells | 10 μM | 14 h | PTEN knockdown significantly increased cell sensitivity to secretion inhibitors BFA and GCA, leading to increased cell death. | Nat Commun. 2018 Jun 19;9(1):2392. |
| Vero cells | 10 μM | 1 hour | GCA treatment resulted in complete dispersal of the Golgi and TGN, similar to the effects of BFA. | Nat Chem Biol. 2009 Mar;5(3):157-65. |
| BEAS-2B bronchial epithelial cells | 4 µM | 24 h | Artificial induction of Golgi fragmentation, reducing bacterial adherence but increasing bacterial replication | Cell Commun Signal. 2023 Aug 17;21(1):208. |
| BEAS-2B bronchial epithelial cells | 4 µM | 4 h | Artificial induction of Golgi fragmentation, reducing bacterial adherence but increasing bacterial replication | Cell Commun Signal. 2023 Aug 17;21(1):208. |
| HEL cells | 10 µM | 48 h | Golgicide A blocked STING exocytosis from HSV-1-infected cells, indicating that STING trafficking through the Golgi is required. | mBio. 2024 Apr 10;15(4):e0037324. |
| BHK-21 cells | 27 μM | 24 h | Evaluate the effect of Golgicide A on DENV NS1 secretion, results showed NS1 secretion was reduced more than 70% in vertebrate cells | J Virol. 2019 Feb 5;93(4):e01985-18. |
| Aag2 cells | 27 μM | 24 h | Evaluate the effect of Golgicide A on DENV NS1 secretion, results showed no effect on NS1 secretion in mosquito cells | J Virol. 2019 Feb 5;93(4):e01985-18. |
| C6/36 cells | 27 μM | 24 h | Evaluate the effect of Golgicide A on DENV NS1 secretion, results showed no effect on NS1 secretion in mosquito cells | J Virol. 2019 Feb 5;93(4):e01985-18. |
| MA104 cells | 10 μM | 12 h | Evaluate the effect of GCA on rotavirus replication, showing a significant reduction in viral yield | J Virol. 2019 Sep 12;93(19):e01062-19. |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/c nude mice | Subcutaneous xenograft model | Subcutaneous injection | 20 mg/kg and 50 mg/kg | Once a week for 4 weeks | Evaluate the inhibitory effect of GCA on tumor growth | Stem Cell Res Ther. 2025 Mar 7;16(1):121 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.52mL 0.70mL 0.35mL |
17.59mL 3.52mL 1.76mL |
35.17mL 7.03mL 3.52mL |
|
| CAS号 | 1139889-93-2 |
| 分子式 | C17H14F2N2 |
| 分子量 | 284.3 |
| SMILES Code | FC1=CC2=C(NC(C3=CC=CN=C3)[C@@]4([H])[C@]2([H])C=CC4)C(F)=C1 |
| MDL No. | MFCD27937048 |
| 别名 | GCA |
| 运输 | 蓝冰 |
| InChI Key | NJZHEQOUHLZCOX-FTLRAWMYSA-N |
| Pubchem ID | 25113626 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 105 mg/mL(369.32 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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