Endocytosis and Dynamin Inhibitors

This article provides an introduction to dynamin and endocytosis and lists the inhibitors that are relevant to research.

Dynamin is an important GTPase enzyme that takes part in different endocytotic processes. It has three major isoforms, and each of these is composed of four primary domains with different functions.

Another major role played by dynamin is in the regulation of the cell cycle. It also has a crucial role in the way centrosomes cohere and in cytokinesis.

Dynamin inhibitors are molecules that inhibit the action of different domains of the dynamin enzyme, and thus prevent the occurrence of endocytosis. They have found wide uses in such areas as the study of the pathways of cell signaling, the cell cycle, cell division, and illnesses such as cancer, infectious diseases, including botulism and HIV, and neurological conditions.

Dynamin Inhibitors

The following is a list of the dynamin inhibitors available:

Name Description Publications featuring our products
Dynole 2-24™ EXCLUSIVE Novel, potent dynamin I and II inhibitor
Dyngo4a™ EXCLUSIVE Novel, highly potent dynamin inhibitor. Dynasore (Asc-192) analog. View
Rhodadyn C10™ EXCLUSIVE Highly potent cell permeable dynamin I inhibitor
Rhodadyn B10™ EXCLUSIVE Negative control for Rhodadyn C10™
Dynole-34-2™ EXCLUSIVE Potent dynamin I and dynamin II inhibitor View
Dynole-31-2™ EXCLUSIVE Negative control for Dynole 34-2™ View
Pitstop 2™ EXCLUSIVE Novel, selective cell permeable clathrin inhibitor View
Iminodyn 17™ Negative control for Iminodyn-22™
Iminodyn 22™ Potent, broad spectrum dynamin inhibitor
RTIL-13™ Potent dynamin I and II inhibitor
MiTMAB™ Cell permeable dynamin I and dynamin II inhibitor View
OctMab™ Cell permeable dynamin I and dynamin II inhibitor
Pro-myristic acid Negative control for MiTMAB™ and OcTMAB™
Dynamin Inhibitors Toolbox Dynamin inhibitor kit from the MiTMAB™, Dynole™ and Iminodyn™ chemical series. View
Dynamin Inhibitors: Iminodyn™ Series Kit Dynamin inhibitor kit from the Iminodyn™ series View
Dynamin Inhibitors: MiTMAB™ Series Kit Dynamin inhibitor kit from the MiTMAB™ series View
Dynamin Inhibitors: Dynole™ Series Kit Dynamin inhibitor kit from the Dynole™ series

A Summary of Dynamin Inhibitor Activity

The following table shows how dynamin inhibitors work via different mechanisms:

Compound Target Domain Dynamin I Inhibition (μM) Dynamin II Inhibition (μM) Synaptic Vesicle Endocytosis (μM) Receptor Mediated Endocytosis (μM) Reference
Dynole-
2-24™
N/A 0.56 5.4 - - Gordon et al 2013
Dyngo-
4a™
N/A 380 nM 2.6 μM Harper et al 2011
Dynole
-34-2™
GAS 1.3 14.2 41.1 5 Hill et al 2009
Dynole-31
-2™
GAS >300 Hill et al 2009
Rhodadyn C10™ N/A 7.1 - - - Robertson et al 2012
Rhodadyn B10™ N/A - - - - Robertson et al 2012
Iminodyn
-22™
GAS 450 nM 390 nM 108 10.7 Hill et al 2010
Iminodyn
-17™
GAS 330 nM 440 nM >300 >300 Hill et al 2010
RTIL-13™ PH 2.3 7.1 9.3 Zhang et al 2008
MiTMAB™ PH 3.1 8.4 2.2 19.9 Hill et al 2004
OcTMAB™ PH 1.9 4.4 6.7 Quan et al 2007
Pro-
Myrisitic Acid
PH 9.2 >300 Quan et al 2007
Dynamin Inhibitors Toolbox PH & GAS
Dynamin Inhibitors: MiTMAB Series Kit PH
Dynole Series Kit GAS
Dynamin Inhibitors: Iminodyn Series Kit GAS

References

  • Hill TA et al. Iminochromene inhibitors of dynamins I and II GTPase activity and endocytosis. J Med Chem 53:4094-102 (2010).
    Read more (PubMed: 20426422)
  • Hill TA et al. Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles. J Med Chem 25:3762-73 (2009).
    Read more (PubMed: 19459681)

Recommended Resources from Our Technical Team

  • Granseth B et al. Clathrin mediated endocytosis: the physiological mechanism of vesicle retrieval at hippocampal synapses. J Physiol 15:681-6 (2007).
    Read more (PubMed: 17599959)
  • Mettlen M et al. Dissecting dynamin's role in clathrin-mediated endocytosis. Pharmacol Ther 47:233-66 (2009)
    Read more (Pubmed: 1975444)

About Abcam

Abcam is a global life sciences company providing highly validated antibodies and other binders and assays to the research and clinical communities to help advance the understanding of biology and causes of disease.

Abcam’s mission is to serve life scientists to help them achieve their mission faster by listening to their needs, continuously innovating and improving and by giving them the tools, data and experience they want. Abcam’s ambition is to become the most influential life science company for researchers worldwide.


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Last updated: Jan 24, 2019 at 11:20 AM

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