Description
Dynasore (304448-55-3) is a noncompetitive inhibitor of dynamin GTPase activity and blocks dynamin-dependent endocytosis in cells, including neurons. It inhibits the GTPase activity of dynamin1, dynamin2, and Drp1 (mitochondrial dynamin). It is cell permeable, fast acting (seconds) and reversible.1,2 Dynasore is a extremely useful tool for studying endocytosis and other cellular events which are dependent on dynamin.3-5
Uses
Dynamin Inhibitor I, Dynasore is an inhibitor of Dynamin I and Dynamin II.
Uses
Dynasore is a cell-permeable, reversible inhibitor of dynamin 1, dynamin 2, and mitochondrial dynamin, Drp1 GTPase activity (IC50 = 15 μM). Through this action, dynasore inhibits clathrin-dependent vesicle formation and endocytosis, which is necessary for internalization of certain parasites and viruses, as well as particles and receptor ligands. In some cases, dynasore can also augment the release of neurotransmitters and secreted cytokines.[Cayman Chemical]
Definition
ChEBI: A carbohydrazide resulting from the formal condensation of the hydrazone moiety of 3,4-dihydroxybenzaldehyde hydrazone with the carboxy group of 3-hydroxy-2-naphthoic acid. It is a cell-permeable, reversible noncompetitive inhibitor of the GTPase activity
f dynamin 1 and 2 and Drp1 (mitochondrial), while exhibiting no significant effect against two other small GTPases, MxA and Cdc42.
Biological Activity
Non-competitive inhibitor of dynamin 1, dynamin 2 and mitochondrial dynamin (Drp1) GTPase activity. Does not inhibit other small GTPases. Blocks endocytic pathways dependent on dynamin and inhibits cell spreading and migration of BSC1 cells.
References
1) Macia et al. (2006), Dynasore, a cell-permeable inhibitor of dynamin; Dev. Cell, 10 839
2) Kirschhausen et al. (2008), Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis; Methods Enzymol., 438 77
3) Lu et al. (2009), Dynamin and activity regulate synaptic vesicle recycling in sympathetic neurons; J. Biol. Chem., 284 1930
4) Chung et al. (2010), Acute dynamin inhibition dissects synaptic vesicle recycling pathways that drive spontaneous and evoked neurotransmission; J. Neurosci., 30 1363
5) Poirer et al. (2009), Dissection of the endogenous cellular pathways of PCSK9-induced low density lipoprotein receptor degradation: evidence for an intracellular route; J. Biol. Chem., 284 28856
