Dynasore

Catalog No.S8047 Batch:S804701

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Technical Data

Formula

C18H14N2O4

Molecular Weight 322.31 CAS No. 304448-55-3
Solubility (25°C)* In vitro DMSO 64 mg/mL (198.56 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

Protocol (from reference)

Kinase Assay:

[1]

  • 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.

Animal Study:

[4]

  • Animal Models

    Female Sprague–Dawley rats

  • Dosages

    1, 10, or 30 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [PLoS One, 2014, 9(4), e94732]

, , Mol Neurobiol. 2017, 54(9):7471-7482

Data from [Data independently produced by , , Virol J, 2016, 13:25.]

Selleck's Dynasore has been cited by 56 publications

Signaling via a CD27-TRAF2-SHP-1 axis during naive T cell activation promotes memory-associated gene regulatory networks [ Immunity, 2024, 57(2):287-302.e12] PubMed: 38354704
Gonococcal OMV-delivered PorB induces epithelial cell mitophagy [ Nat Commun, 2024, 15(1):1669] PubMed: 38396029
Repurposing a tricyclic antidepressant in tumor and metabolism disease treatment through fatty acid uptake inhibition [ J Exp Med, 2023, 220(3)e20221316] PubMed: 36520461
SAMHD1-induced endosomal FAK signaling promotes human renal clear cell carcinoma metastasis by activating Rac1-mediated lamellipodia protrusion [ Exp Mol Med, 2023, 55(4):779-793] PubMed: 37009792
RAGA prevents tumor immune evasion of LUAD by promoting CD47 lysosome degradation [ Commun Biol, 2023, 6(1):211] PubMed: 36823443
Regulated dynamic subcellular GLUT4 localization revealed by proximal proteome mapping in human muscle cells [ J Cell Sci, 2023, 136(23)jcs261454] PubMed: 38126809
Porcine deltacoronavirus enters ST cells by clathrin-mediated endocytosis and does not require Rab5, Rab7, or Rab11 [ Microbiol Spectr, 2023, 10.1128/spectrum.02553-23] PubMed: 37962380
Low-dose metformin targets the lysosomal AMPK pathway through PEN2 [ Nature, 2022, 603(7899):159-165] PubMed: 35197629
The aldolase inhibitor aldometanib mimics glucose starvation to activate lysosomal AMPK [ Nat Metab, 2022, 4-10:1369-1401] PubMed: 36217034
α-Synuclein-containing erythrocytic extracellular vesicles: essential contributors to hyperactivation of monocytes in Parkinson's disease [ J Neuroinflammation, 2022, 19(1):53] PubMed: 35193594

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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