All tags Agonists-activators-antagonists-and-inhibitors Dynamin and endocytosis inhibitors

Dynamin and endocytosis inhibitors

An introduction to dynamin and endocytosis with a simple reference guide of inhibitors for your research.

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 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.


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Contents


Dynamin inhibitors available 

Name
DescriptionPublications featuring our products
Dynole 2-24™EXCLUSIVENovel, potent dynamin I and II inhibitor
Dyngo4a™EXCLUSIVENovel, highly potent dynamin inhibitor. Dynasore (Asc-192) analog.View
Rhodadyn C10™EXCLUSIVEHighly potent cell permeable dynamin I inhibitor
Rhodadyn B10™EXCLUSIVENegative control for Rhodadyn C10™
Dynole-34-2™EXCLUSIVEPotent dynamin I and dynamin II inhibitorView
Dynole-31-2™EXCLUSIVENegative control for Dynole 34-2™View
Pitstop 2™EXCLUSIVENovel, selective cell permeable clathrin inhibitorView
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 inhibitorView
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™ seriesView
Dynamin Inhibitors: MiTMAB™ Series Kit
Dynamin inhibitor kit from the MiTMAB™ seriesView
Dynamin Inhibitors: Dynole™ Series Kit
Dynamin inhibitor kit from the Dynole™ series



Dynamin inhibitors activity summary

Comp-

ound

Target DomainDynamin I Inhibition (μM)Dynamin II Inhibition (μM)

Synaptic Vesicle Endocyto

-sis (μM)

Recept-or Mediated Endocyto

-sis (μM)

Refere

-nce

Dynole-
2-24™

N/A0.565.4--Gordon et al 2013

Dyngo-
4a™

N/A380 nM2.6 μM

Harper et al 2011
Dynole
-34-2™
GAS1.314.241.15Hill et al 2009
Dynole-31
-2™
GAS>300


Hill et al 2009
Rhodadyn C10™N/A7.1---Robertson et al 2012
Rhodadyn B10™N/A----Robertson et al 2012
Iminodyn
-22™
GAS450 nM390 nM10810.7Hill et al 2010
Iminodyn
-17™
GAS330 nM440 nM>300>300Hill et al 2010
RTIL-13™PH2.3
7.19.3Zhang et al 2008
MiTMAB™PH3.18.42.219.9Hill et al 2004
OcTMAB™PH1.94.4
6.7Quan et al 2007
Pro-
Myrisitic Acid
PH9.2

>300Quan et al 2007
Dynamin Inhibitors ToolboxPH & GAS




Dynamin Inhibitors: MiTMAB Series KitPH




Dynole Series KitGAS




Dynamin Inhibitors: Iminodyn Series KitGAS





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)


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