Dynasore

"目录号: HY-15304

Cytoskeleton-

Dynasore 是dynaminGTPase活性的抑制剂，IC50值为15 μM。

Dynamin

相关产品

Mdivi-1-

生物活性

Description

Dynasore is an inhibitor of the GTPase activity ofdynaminwith anIC50of 15 μM.

IC50& Target

IC50: 15 μM (GTPase activity of dynamin1 and 2)[1]

In Vitro

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[1]. 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[2]. 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 adult mouse cardiomyocytes subjected to oxidative stress, dynasore increases cardiomyocyte survival and viability[3].

In Vivo

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[4].

References

[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.