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.
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 | ||||||
---|---|---|---|---|---|---|
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 |
Endocytosis and exocytosis products
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)»