Dynamin inhibitors - @ a glance

Dynamin is a key GTPase involved in various forms of endocytosis and is comprised of 3 major isoforms, all of which have four main functional domains.

In addition to being a key component of endocytosis, dynamin participates in cell cycle progression and has also been shown to have critical roles in centrosome cohesion and cytokinesis.

Dynamin inhibitors inhibit different domains of dynamin, leading to the subsequent inhibition of endocytosis. Consequently, the dynamin inhibitors have wide-spread application allowing investigation of cell signalling pathways, the cell cycle and cellular division, in addition to other medical conditions such as cancer, neurological conditions and infectious diseases such as botulism and HIV.

Dynamin has four main functional domains; the GTPase, Pleckstrin homology (PH), Assembly domain (AD)and Proline rich domain (PRD). Different dynamin inhibitors target various sites of dynamin.

Dynamin inhibitors summary

IC50
Compound Target
Domain		 Dynamin I
Inhibition (μM)		 Dynamin II
Inhibition (μM)		 Synaptic Vesicle
Endocytosis
Endocytosis (μM)		 Receptor Mediated
Endocytosis
Inhibition (μM)		 Reference
Iminodyn-22™ GAS 450 390 108 10.7 Hill et al 2010
Imminodyn-17™ GAS 330 440 >300 >300 Hill et al 2010
Dynole-34-2™ GAS 1.3 14.2 41.1 5 Hill et al 2009
Dynole-31™ GAS >300 Hill et al 2009
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
Dyngo-4a™ N/A 380 nM 2.6 nM >300 Harper et al 2011
Dynamin Inhibitors Toolbox PH & GAS
Dynamin Inhibitors: MiTMAB Series Kit PH
Dynamin Inhibitors: Dynole Series Kit GAS
Dynamin Inhibitors: Iminodyn Series Kit GAS

References

  1. Hill et al (2010) Iminochromene inhibitors of dynamins I and II GTPase activity and endocytosis. J Med Chem. 53:4094-102. Abstract
  2. Hill et al (2009) Inhibition of dynamin mediated endocytosis by the dynoles--synthesis and functional activity of a family of indoles. J Med Chem. 25:3762-73. Abstract
  3. Doherty and McMahon (2009) Mechanisms of endocytosis. Annu Rev Biochem. 78:857-902. Abstract

Recommended reviews from our technical team

  1. Doherty and McMahon (2009) Mechanisms of endocytosis. Annu Rev Biochem. 78:857-902. Abstract
  2. Granseth et al (2007) Clathrin mediated endocytosis: the physiological mechanism of vesicle retrieval at hippocampal synapses. Abstract
  3. Mettlen et al (2009) Dissecting dynamin's role in clathrin-mediated endocytosis. Abstract

Technical resources

Endocytosis - @ a glance

Clathrin inhibitors - @ a glance

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