Dynasore

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Chemical Structure| 304448-55-3 同义名 : -
CAS号 : 304448-55-3
货号 : A209594
分子式 : C18H14N2O4
纯度 : 98%
分子量 : 322.315
MDL号 : MFCD00292551
存储条件：

Pure form Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

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

DMSO: 50 mg/mL(155.13 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：

5% DMSO+30% PEG 300+5% Tween 80+water 4 mg/mL

生物活性
靶点

  • Dynamin

    Dynamin1/2, IC50:~15 μM
描述 Dynasore impedes the GTPase activities of dynamin1, dynamin2, and Drp1 (mitochondrial dynamin) specifically, without affecting other small GTPases. It serves as an effective suppressor of endocytic pathways that rely on dynamin, by promptly obstructing the formation of coated vesicles immediately following its introduction. Throughout the treatment with Dynasore, an accumulation of two distinct forms of coated pit intermediates occurs: g-shaped, partially formed pits, and O-shaped, completely formed pits, observed at the moment of detachment[1]. Furthermore, Dynasore effectively blocks the infection of human epithelial and neuronal cells by HSV-1 and HSV-2, encompassing cells from the primary genital tract as well as human fetal neurons and astrocytes. It diminishes the quantity of viral capsids reaching the nuclear pore when administered at the initiation of viral entry, and, if applied up to 8 hours after entry, Dynasore obstructs the transport of newly synthesized viral proteins from the nucleus to the cytosol[2]. In the context of ischemia/reperfusion, Dynasore prevents the elevation of left ventricular end-diastolic pressure and curtails cardiac troponin I release during reperfusion, contributing to a reduction in infarct size. When adult mouse cardiomyocytes are exposed to oxidative stress, Dynasore enhances cell survival and viability[3].
作用机制 Dynasore acts as a noncompetitive inhibitor of dynamin by blocking the basal and stimulated rates of GTP hydrolysis mediated by isolated GTPase domain of dynamin, thereby impeding clathrin-mediated endocytosis in cells.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
COS7 cells Function assay Inhibition of transferrin uptake in african green monkey COS7 cells by microscopic TexasRed imaging, IC50=15 μM 20621477
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.10mL

0.62mL

0.31mL

15.51mL

3.10mL

1.55mL

31.03mL

6.21mL

3.10mL
参考文献

[1]Macia E, et al. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50.

[2]Mues MB, et al. Dynasore disrupts trafficking of herpes simplex virus proteins. J Virol. 2015 Jul;89(13):6673-84.

[3]Gao D, et al. Dynasore protects mitochondria and improves cardiac lusitropy in Langendorff perfused mouse heart. PLoS One. 2013 Apr 15;8(4):e60967.

[4]Li G, et al. Dynasore Improves Motor Function Recovery via Inhibition of Neuronal Apoptosis and Astrocytic Proliferation after Spinal Cord Injury in Rats. Mol Neurobiol. 2016 Nov 7.