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CAS No.: 1256493-34-1

Hydroxy-Dynasore Catalog No. CSN19185

Synonyms: Dyngo-4a

Hydroxy Dynasore is an inhibitor of dynamin1 and dynamin2 with IC50 of 0.38 μM and 2.6 µM respectively. It can prevent dynamin-mediated endocytosis in multiple cell types.

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技术信息

生物活性

描述Dynamin is a large GTPase enzyme that severs membrane‐bound clathrin‐coated vesicles. Dyngo-4a inhibits both dynamin I and II with IC50s for sheep brain dynamin I of 380 ± 0.05 nM (n = 5) and for recombinant rat dynamin II of 2.3 ± 0.2 μM (n = 3). It inhibits dynamin‐dependent endocytosis of transferrin in multiple cell types with IC₅₀ value of 5.7 μM. Inhibition of non‐neuronal clathrin‐mediated endocytosis (CME) was observed with as little as 5‐min preincubation with 10 μM Dyngo-4a in U2OS cells. 70% of normal non‐neuronal CME levels was observed at ten minutes after the removal of 10 μM 4a indicating its endocytic block activity was rapid and reversible ^[3]. The ability of Dyngo-4a to prevent the muscle paralysis induced by purified BoNT/A was tested in a rat hemidiaphragm twitch model. Both the decline in contraction and the time to reach 50% of decline were significantly increased in the Dyngo-4a-treated muscles compared with the BoNT/A control group demonstrating that Dyngo-4a provides significant protection against BoNT/A-induced muscle paralysis. CD-1 mice were given an intraperitoneal injection of Dyngo-4a (1 mg) or vehicle followed by a booster 4.5–8 h later. Mice injected with Dyngo-4a took significantly longer to exhibit clear signs of botulism, 860 ± 65 min compared with 656 ± 55 min indicating that Dyngo-4a pretreatment provides significant protection against botulism ^[4].
参考文献

[1] McCluskey A, Daniel JA, et al. Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic. 2013 Dec;14(12):1272-89.
[2] Harper CB, Martin S, et al. Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism. J Biol Chem. 2011 Oct 14;286(41):35966-76.
[3] McCluskey A, Daniel JA, Hadzic G, Chau N, Clayton EL, Mariana A, Whiting A, Gorgani NN, Lloyd J, Quan A, Moshkanbaryans L, Krishnan S, Perera S, Chircop M, von Kleist L, McGeachie AB, Howes MT, Parton RG, Campbell M, Sakoff JA, Wang X, Sun JY, Robertson MJ, Deane FM, Nguyen TH, Meunier FA, Cousin MA, Robinson PJ. Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic. 2013 Dec;14(12):1272-89. doi: 10.1111/tra.12119. Epub 2013 Oct 9. PMID: 24025110; PMCID: PMC4138991.
[4] Harper CB, Martin S, Nguyen TH, Daniels SJ, Lavidis NA, Popoff MR, Hadzic G, Mariana A, Chau N, McCluskey A, Robinson PJ, Meunier FA. Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism. J Biol Chem. 2011 Oct 14;286(41):35966-35976. doi: 10.1074/jbc.M111.283879. Epub 2011 Aug 5. PMID: 21832053; PMCID: PMC3195592.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9558 mL
- 14.7792 mL
- 29.5583 mL
- 5 mM
- 0.5912 mL
- 2.9558 mL
- 5.9117 mL
- 10 mM
- 0.2956 mL
- 1.4779 mL
- 2.9558 mL

技术信息

CAS号

1256493-34-1

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H14N2O5

运输

蓝冰

分子量

338.31

别名

Dyngo-4a

溶解度

DMSO	85.0 mg/mL (251.2 mM)
Water	insoluble

动物实验配方

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