Dynasore
Dynasore is a noncompetitive inhibitor of GTPases with the IC50 value of 15 μM[1] [2].
GTPases (singular GTPase) are hydrolase enzymes that play an important role in GTP binding and hydrolyzing. GTPases involve in many processes, like, transduction signal, protein biosynthesis, translocation proteins through membranes, and transporting vesicles within the cell. It has been reported that dynasore could inhibit the GTPase activity of dynamin1, dynamin2 and Drp1 [3] [4].
Dynasore is a potent GTPases inhibitor and functions on the sites of dynamin1, dynamin2 or Drp1. When tested with HL-1 cells, treated cells with dynasore blocked the endocytic process via inhibiting the activity of dynamin [1]. Using genetically encoded pH-sensitive fluorescent probe synaptopHluorin to study the role of dynasore in the synapses expressing spH, and the results showed that dyansore treatment resulted in the normal stimulus-triggered increase in fluorescence intensity via reducing the GTPase activity of dynamin which in turn blocked the synaptic endocytosis[4]. Dynasore worked as inhibitor of dynamin GTPase activity which blocks dynamin-dependent endocytosis not only in cells, but also including neurons [3].
References:
[1].Zheng, J., et al., Chymase mediates injury and mitochondrial damage in cardiomyocytes during acute ischemia/reperfusion in the dog. PLoS One, 2014. 9(4): p. e94732.
[2].McCluskey, A., et al., Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic, 2013. 14(12): p. 1272-89.
[3].Kirchhausen, T., E. Macia, and H.E. Pelish, Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis. Methods Enzymol, 2008. 438: p. 77-93.
[4].Newton, A.J., T. Kirchhausen, and V.N. Murthy, Inhibition of dynamin completely blocks compensatory synaptic vesicle endocytosis. Proc Natl Acad Sci U S A, 2006. 103(47): p. 17955-60.
- 1. Wei P, Ning M, et al. "Spiroplasma eriocheiris entered Drosophila Schneider 2 cells and relied on clathrin-mediated endocytosis and macropinocytosis." Infect Immun. 2019 Aug 26. pii: IAI.00233-19. PMID:31451616
- 2. Ying Wen, Shouwen Chen, et al."Dysregulated haemolysin promotes bacterial outer membrane vesicles‐induced pyroptotic‐like cell death in zebrafish."Cellular Microbiology. 31 January 2019.
- 3. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525
- 4. Mai J, Li X, et al. "A DNA Thioaptamer with Homing Specificity to Lymphoma Bone Marrow Involvement." Mol Pharm. 2018 May 7;15(5):1814-1825. PMID:29537266
- 5. Schappe MS, Szteyn K, et al."Chanzyme TRPM7 Mediates the Ca(2+) Influx Essential for Lipopolysaccharide-Induced Toll-Like Receptor 4 Endocytosis and Macrophage Activation." Immunity. 2018 Jan 16;48(1):59-74.e5. PMID:29343440
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 322.31 |
Cas No. | 304448-55-3 |
Formula | C18H14N2O4 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥16.12 mg/mL in DMSO |
Chemical Name | (E)-N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide |
SDF | Download SDF |
Canonical SMILES | OC1=C(C(N/N=C/C(C=C2)=CC(O)=C2O)=O)C=C(C=CC=C3)C3=C1 |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment [1]: | |
Cell lines |
Hela cells |
Preparation method |
The solubility of this compound in DMSO is > 16.1 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
Reacting condition |
0, 1, 10, 20, 40, 60 and 80 μM; 30 mins |
Applications |
In Hela cells preincubated with 80 μM Dynasore for 30 mins, the uptake, trafficking and intracellular accumulation of transferrin were all significantly blocked. Moreover, Dynasore dose-dependently inhibited transferrin uptake. In addition, the effect of Dynasore on transferrin uptake was proved to be reversible. |
References: [1]. Macia E, Ehrlich M, Massol R, Boucrot E, Brunner C, Kirchhausen T. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50. |
Description | Dynasore is a cell-permeable and noncompetitive inhibitor of the GTPase activity of dynamin with IC50 value of 15 µM. | |||||
Targets | dynamin GTPase | |||||
IC50 | 15 µM |
Quality Control & MSDS
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Chemical structure

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