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Dyngo-4a Sale

(Synonyms: Dyngo-4a) 目录号 : GC17208

An inhibitor of dynamin

Dyngo-4a Chemical Structure

Cas No.:1256493-34-1

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Sample solution is provided at 25 µL, 10mM.

Description

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.

实验参考方法

Kinase experiment [1]:

Kinase assays

For analysis of the kinetics of inhibition, dynamin I at a final concentration of 17 nM was incubated with GTPase buffer containing PS (2 μg/mL) and varying amounts of GTP (50–250 μM) in the presence of 4a at a concentration range between 0.5 and 6 μM. The reaction was stopped after 30 min by addition of EDTA (0.5 mM, pH7.4).

Cell experiment [1]:

Cell lines

U2OS cell lines

Preparation method

Soluble in DMSO. 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.

Reacting condition

1~100 μM

Applications

Dyngo-4a potently inhibited Tfn endocytosis with IC50 values of 5.7±1.0 μM, approximating the activity of the most potent small molecule endocytosis inhibitors previously reported.

Animal experiment [2]:

Animal models

Female CD-1 mice

Dosage form

30 mg/kg, intraperitoneal injection

Application

Mice injected with Dyngo-4a took significantly longer to exhibit clear signs of botulism which indicates that Dyngo-4a pretreatment provides significant protection against botulism.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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.

化学性质

Cas No. 1256493-34-1 SDF
别名 Dyngo-4a
化学名 (E)-N'-(2,3,4,5-tetrahydroxybenzylidene)-2-naphthohydrazide
Canonical SMILES O=C(C1=CC=C2C=CC=CC2=C1)N/N=C/C3=CC(O)=C(O)C(O)=C3O
分子式 C18H14N2O5 分子量 338.31
溶解度 ≥ 33.8mg/mL in DMSO 储存条件 Store at -20°C
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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。
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。

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1 mg 5 mg 10 mg
1 mM 2.9559 mL 14.7793 mL 29.5587 mL
5 mM 0.5912 mL 2.9559 mL 5.9117 mL
10 mM 0.2956 mL 1.4779 mL 2.9559 mL
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