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Golgicide A

现货
Catalog No.
B1385
GBF1抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
现货
5mg
¥ 680.00
现货
25mg
¥ 2,590.00
现货

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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].
References:
[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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt284.3
Cas No.1139889-93-2
FormulaC17H14F2N2
Solubility≥12.95mg/mL in DMSO
Chemical Name(3aS,9bR)-6,8-difluoro-4-(pyridin-3-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
SDFDownload SDF
Canonical SMILESFC(C=C12)=CC(F)=C2NC(C3=CN=CC=C3)[C@]4([H])[C@@]1([H])C=CC4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人肝癌细胞系Huh7(电转J6 / JFH1 RNA并转染编码NS5A的质粒的Huh7.5细胞)。

溶解方法

在DMSO的溶解度>13mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10μM分别处理4,24和48小时。

应用

Golgicide A是一种特异性抑制GBF1的药物,已被证明可以降低HCV(丙型肝炎病毒)RNA复制。用golgicide A处理细胞减少了JFH1-HCVcc细胞系统中的Arf1(ADP-核糖基化因子1)和HCV RNA水平。在J6 / JFH1细胞中,一些病毒NS蛋白从斑点状的细胞器迁移到LD的周围,以响应Golgicide A对Arf1的抑制。Golgicide A处理还降低了HCV RNA水平,并引起NS5A(非结构蛋白)的再分布和感染性病毒颗粒的积累。

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.

质量控制

质量控制和MSDS

批次:

化学结构

Golgicide A