304448-55-3

Usage

Uses

Used in Cellular Research:
Dynasore is used as a research tool for studying endocytosis and other cellular events that are dependent on dynamin. Its ability to inhibit clathrin-dependent vesicle formation and endocytosis makes it a valuable asset in understanding the underlying mechanisms of these processes.
Used in Neuroscience:
In the field of neuroscience, Dynasore is used as an inhibitor of Dynamin I and Dynamin II, which are essential proteins involved in the regulation of neurotransmitter release. By inhibiting these proteins, researchers can gain insights into the role of dynamin in synaptic vesicle recycling and neurotransmission.
Used in Antiviral and Antimicrobial Research:
Dynasore is used as an inhibitor to study the internalization of certain parasites and viruses, as well as particles and receptor ligands. Its ability to block endocytosis can provide valuable information on the mechanisms by which these pathogens enter and infect host cells.
Used in Drug Delivery Systems:
In the development of drug delivery systems, Dynasore can be employed to enhance the release of neurotransmitters and secreted cytokines. This application can be particularly useful in the design of targeted drug delivery systems that aim to improve the bioavailability and therapeutic outcomes of various medications.

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

Upstream product

• 5341-58-2 3-hydroxy-2-naphthohydrazide 
• 139-85-5 3,4-dihydroxybenzaldehyde 

Relevant academic research and scientific papers

Synthesis of potent chemical inhibitors of dynamin GTPase

Dynamin is a key regulatory protein in clathrin mediated endocytosis. Compared to genetic or immunological tools, small chemical dynamin inhibitors such as dynasore have the potential to study the dynamic nature of endocytic events in cells. Dynasore inhibits dynamin GTPase activity and transferrin uptake at IC50 ～15 μM but use in some biological applications requires more potent inhibitor than dynasore. Here, we chemically modified the side chains of dynasore and found that two derivatives, DD-6 and DD-11 more potently inhibited transferrin uptake (IC50: 4.00 μM for DD-6, 2.63 μM for DD-11) and dynamin GTPase activity (IC50: 5.1 μM for DD-6, 3.6 μM for DD-11) than dynasore. The effect was reversible and they were washed more rapidly out than dynasore. TIRF microscopy showed that they stabilize the clathrin coats on the membrane. Our results indicated that new dynasore derivatives are more potent inhibitor of dynamin, displaying promise as leads for the development of more effective analogues for broader biological applications.