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Dyngo-4a

现货
Catalog No.
B5997
动力蛋白抑制剂
组合的产品项目
规格价格库存 数量
10mg
¥ 850.00
现货
50mg
¥ 2,450.00
现货
200mg
¥ 4,900.00
现货

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Background

Target: DynI (brain); DynI (rec); DynII (rec)

IC50: 0.38 μM; 1.1 μM; 2.3 μM

Dyngo-4a is a potent, novel dynamin inhibitor with IC50 values of 0.38 μM, 1.1 μM, and 2.3 μM for DynI (brain), DynI (rec), and DynII (rec), respectively [1]. Dynamin is a large GTPase enzyme that severs as membrane-bound clathrin-coated vesicles [1].

In vitro: Dyngo-4a (100 μM) caused a reduction in β-catenin levels in human colon carcinoma RKO cells [2]. In addition, Dyngo-4a prevented the uptake of BoNT/A-Hc and blocked BoNT/A-induced SNAP25 cleavage in cultured hippocampal neurons [3]. Dyngo-4a is potent, reversible endocytosis inhibitor in non-neuronal cells. Dyngo-4a inhibited synaptic vesicle endocytosis (SVE) in synaptosomes and neurons with an IC50 value of 26.8 μM [1].

In vivo: Dynamin is a potential therapeutic target for counteracting botulism. Dyngo-4a (30 mg/kg, intraperitoneal injection) treatment suppressed BoNT/A-induced muscle paralysis at the rat hemidiaphragm and significantly delayed the onset of botulism in an in vivo murine model [3].

References:
1.  McCluskey A, Daniel JA, Hadzic G, Chau N, Clayton EL, Mariana A, et al. Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic. 2013;14(12):1272-89.
2.  Gagliardi M, Hernandez A, McGough IJ, Vincent JP. Inhibitors of endocytosis prevent Wnt/Wingless signalling by reducing the level of basal beta-catenin/Armadillo. J Cell Sci. 2014;127(Pt 22):4918-26.
3.  Harper CB, Martin S, Nguyen TH, Daniels SJ, Lavidis NA, Popoff MR, et al. Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism. J Biol Chem. 2011;286(41):35966-76.

Chemical Properties

StorageStore at -20°C
M.Wt338.31
Cas No.1256493-34-1
FormulaC18H14N2O5
Solubility≥33.8mg/mL in DMSO
Chemical Name(E)-N'-(2,3,4,5-tetrahydroxybenzylidene)-2-naphthohydrazide
SDFDownload SDF
Canonical SMILESO=C(C1=CC=C2C=CC=CC2=C1)N/N=C/C3=CC(O)=C(O)C(O)=C3O
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

酶学实验[1]:

激酶检测

为了分析抑制动力学,将终浓度为17nM的dynamin I与含有PS(2μg/mL)的GTPase缓冲液和不同量的GTP(50-250μM)以及不同浓度的Dyngo-4a(0.5~6μM)孵育。30分钟后,加入EDTA(0.5mM,pH 7.4)停止反应。

细胞实验[1]:

细胞系

U2OS细胞系

溶解方法

可溶于DMSO。为了获得更高浓度,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

1~100 μM

应用

Dyngo-4a有效抑制Tfn内吞作用,IC50值为5.7±1.0μM,近似于有报道的最有效的小分子内吞抑制剂的活性。

动物实验[2]:

动物模型

雌性CD-1小鼠

剂量

30 mg/kg,腹腔注射

应用

用Dyngo-4a注射的小鼠花费更长的时间来表现出明显的肉毒中毒症状,这表明Dyngo-4a预处理提供了显著的防止肉毒中毒的保护作用。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] McCluskey A, Daniel JA, Hadzic G, Chau N, Clayton EL, Mariana A, et al. Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic. 2013;14(12):1272-89.

[2] Harper CB, Martin S, Nguyen TH, Daniels SJ, Lavidis NA, Popoff MR, et al. Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism. J Biol Chem. 2011;286(41):35966-76.

质量控制

化学结构

Dyngo-4a