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Dynasore

Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).

Dynasore Chemical Structure

Dynasore Chemical Structure

CAS No. 304448-55-3

Purity & Quality Control

Dynasore Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 cells Function assay Inhibition of transferrin uptake in african green monkey COS7 cells by microscopic TexasRed imaging, IC50=15 μM 20621477
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Biological Activity

Description Dynasore is a cell-permeable, reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, also inhibits the mitochondrial dynamin Drp1, with no effect against other small GTPase. Dynasore suppresses mTORC1 activity and induces autophagy. Dynasore inhibits the entry of several viruses, including herpes simplex virus (HSV).
Targets
Dynamin1/2 [1]
(Cell-free assay)
~15 μM
In vitro
In vitro

Dynasore acts as a potent inhibitor of endocytic pathways known to depend on dynamin by rapidly blocking coated vesicle formation within seconds of dynasore addition. Two types of coated pit intermediates accumulate during dynasore treatment, U-shaped, half formed pits and O-shaped, fully formed pits, captured while pinching off. Dynasore at concentration of 80 μM, also inhibits the enzymatic activity of the mitochondrial dynamin Drp1. Dynasore strongly blocks the uptake, trafficking, and intracellular accumulation of transferrin in HeLa cells with IC50 of ~15 μM. Dynasore also prevents the endocytosis of low-density lipoprotein and cholera toxin. Dynasore (80 μM) strongly interferes with the spread of freshly plated cells, and inhibits BSC1 cells migration by about 50%. [1]

Dynasore completely and reversibly blocks endocytosis in cultured hippocampal neurons after sustained or brief action potentials stimuli with full inhibition at 80 μM and a half-maximal inhibition at ~30 μM. In the presence of Dynasore, low-frequency stimulation leads to sustained accumulation of synaptopHluorin and other vesicular proteins on the surface membrane at a rate predicted from net exocytosis, as well as a reduction in the density of synaptic vesicles and the presence of endocytic structures only at synapses. [2]

Dynasore can block human epithelial cell HEK 293 infection of human papillomavirus type 16 and bovine papillomavirus type 1 pseudovirions with equal IC50 of ~80 μM, which is partly reversible. [3]
Kinase Assay GTPase activity assay
GTPase activity is measured by using a radioactive charcoal-based assay. Proteins dynamin, human Drp1 at the indicated concentrations are incubated in 10 mM Tris (pH 7.2), 2 mM MgCl2, and 20 μM GTPγP32 (2000 dpm/pmol) alone or, when appropriate, with lipid nanotubes for the indicated times and temperatures; the final NaCl concentration is 150 mM NaCl for the high-salt condition and between 10 and 20 mM for the low-salt conditions depending on the protein concentration in the stock solution. GTP hydrolysis is ended by transferring 10 μL aliquots of the reaction into a 500 μL slurry containing acid-washed charcoal, followed by a 10 min centrifugation (20000 × g, 4 ℃) and final counting of the liberated P32O4 contained in 250 μL supernatant.
Experimental Result Images Methods Biomarkers Images PMID
Western blot CCND1 / CDK4 / p-JAK2 / JAK2 / p-STAT3 / STAT3 p-MET / MET 31534119
Immunofluorescence STAT3 / p-STAT3 31534119
Growth inhibition assay Cell viability 31534119

Chemical Information & Solubility

Molecular Weight 322.31 Formula

C18H14N2O4
CAS No. 304448-55-3 SDF Download Dynasore SDF
Smiles C1=CC=C2C=C(C(=CC2=C1)C(=O)NN=CC3=CC(=C(C=C3)O)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 64 mg/mL ( (198.56 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

Question 1:
How to reconstitute the compound for in vivo use? Could you please advise a solution for ip please?

Answer:
The IP formula for S8047 is 5% DMSO+30%PEG 300+5% Tween 80+ddH2O.

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