Dynasore

Catalog No.S8047

Dynasore Chemical Structure

Molecular Weight(MW): 322.31

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.

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3 Customer Reviews

  • Effects of dynasore on active caspase-3 expression at 3 days after SCI. c) Active caspase-3/NeuN/DAPI double labeling. Scale bars = 100 μm.

    Mol Neurobiol, 2016.. Dynasore purchased from Selleck.

    Effects of dynasore and NH 4 Cl on GCRV entry. GCRV-JX01 virions at an MOI of 20 were adsorbed to CIK cells that had been pretreated with (a) DMSO(condition equal to the volume of dynasore used for the 50 μM), (b) 50 μM dynasore in DMSO or (c) 20 mM ammonium chloride (NH4Cl) in water. After 1 h of viral adsorption at 0 °C, warm medium with inhibitors described above was quickly added. At 30 min post-infection (mpi), non-internalized viruses were removed and washed three times with PBS. Then cells were fixed with 4 % paraformaldehyde and permeabilized with 0.1 % Triton X-100 for 10 min at room temperature. The samples were labeled with an anti-GCRV VP5 polyantibody (green) and DAPI (Blue). Scale bars represent 20 μM

    Virol J, 2016, 13:25.. Dynasore purchased from Selleck.

  • Immunocytochemistry demonstrates NR4A1 nuclear location at control (non-chymase treated) in HL-1 cells (a). Chymase (2.5 ug/ml) treatment for 2 h induces NR4A1 (red) cytoplasmic translocation in HL-1 cells as well as myosin (green) disruption (panel b). Active chymase enters HL-1 cells and is prevented by Dynasore (c and d). There marked entry into HL-1 cell nuclei and cytoplasm after treatment with chymase (5 ug/ml) for 2 h that is prevented by pre-treatment with Dynasore. Lack of co-staining with caveolin 3 (green) demonstrates that chymase is not transported via caveolae. Dynasore prevents transferrin uptake in HL-1 cells.

    PLoS One 2014 9(4), e94732. Dynasore purchased from Selleck.

Purity & Quality Control

Choose Selective Dynamin Inhibitors

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.
Targets
Dynamin1/2 [1]
(Cell-free assay)
~15 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 cells MU\GeY5kfGmxbjDhd5NigQ>? NVSyTINCUW6qaXLpeIlwdiCxZjD0doFve2[ncoLpckB2eHSja3WgbY4h[W[{aXPhckBoemWnbjDtc45s\XliQ1;TO{Bk\WyuczDifUBucWO{b4Pjc5Bq[yCWZYjhd3Jm\CCrbXHnbY5oNCCLQ{WwQVE2KM7:TR?= NYjkZ2pEOjB4MkG0O|c>

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro DMSO 64 mg/mL (198.56 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 322.31
Formula

C18H14N2O4

CAS No. 304448-55-3
Storage powder
Synonyms N/A

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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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID