Dynamin inhibitors - @ a glance

At a glance guides

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.

 

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Dynamin inhibitors inhibit different domains of dynamin, leading to 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 inhibitors now available

 

Name  Description Biological data 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 View
 

Dynamin inhibitors activity summary

  IC50 
CompoundTarget DomainDynamin 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
 

Endocytosis and exocytosis products

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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) »

Doherty GJ and McMahon HT. Mechanisms of endocytosis. Annu Rev Biochem 78:857-902 (2009). 
Read more (PubMed: 19317650) »

 

Recommended resources from our technical team

Doherty GJ and McMahon HT. Mechanisms of endocytosis. Annu Rev Biochem 78:857-902 (2009).
Read more (PubMed: 19317650) »

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)»

 

Endocytosis & exocytosis technical resources

Endocytosis - @ a glance »

Clathrin inhibitors - @ a glance »

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