Hydroxy-Dynasore

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Chemical Structure| 1256493-34-1 同义名 : Dyngo-4a
CAS号 : 1256493-34-1
货号 : A511904
分子式 : C18H14N2O5
纯度 : 99%+
分子量 : 338.314
MDL号 : MFCD23704787
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(147.79 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
动物实验配方：
生物活性
靶点

  • Dynamin

    DynI (rec), IC50:2.3 μM

    DynI (brain), IC50:0.38 μM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.78mL

2.96mL

1.48mL

29.56mL

5.91mL

2.96mL
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.