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抑制剂描述:

产品名称:Dynasore

产品别名:见爱必信

英文别名:Dynasore

靶点:Dynamin

CAS:304448-55-3

纯度:>98%

外观:见爱必信

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Dynasore is a cell-permeable small molecule that inhibits the GTPase activity of dynamin1, dynamin2 and Drp1, the mitochondrial dynamin.

溶解性:DMSO : 32.2 mg/mL (100 mM)
Ethanol : 1.6 mg/mL (5 mM)

体外研究:

Dynasore interferes with the GTPase activity of dynamin1, dynamin2, and Drp1, the mitochondrial dynamin, but not of other small GTPases. Dynasore acts as a potent inhibitor of endocytic pathways known to depend on dynamin by rapidly blocking coated vesicle formation within seconds of dynasore addition. Two types of coated pit intermediates accumulate during dynasore treatment, g-shaped, half formed pits and O-shaped, fully formed pits, captured while pinching off. Dynasore inhibits HSV-1 and HSV-2 infection of human epithelial and neuronal cells, including primary genital tract cells and human fetal neurons and astrocytes. Dynasore reduces the number of viral capsids reaching the nuclear pore if added at the time of viral entry and that, when added as late as 8 h postentry, dynasore blocks the transport of newly synthesized viral proteins from the nucleus to the cytosol. Dynasore prevents ischemia/reperfusion induced elevation of left ventricular end diastolic pressure. Dynasore also decreases cardiac troponin I efflux during reperfusion and reduces infarct size. In cultured adul mouse cardiomyocytes subjected to oxidative stress, dynasore increases cardiomyocyte survival and viability.

体内研究:Dynasore ameliorates the motor dysfunction greatly at 3, 7, and 10 days after SCI in rats. Dynasore significantly enhances motor function which may be by inhibiting the activation of neuronal mitochondrial apoptotic pathway and astrocytic proliferation in rats after SCI.

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