Dynasore

For research use only.

Catalog No.S8047

25 publications

Dynasore Chemical Structure

CAS No. 304448-55-3

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).

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Selleck's Dynasore has been cited by 25 publications

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. 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
COS7 cells M1\2TmZ2dmO2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKHS{YX7z[oVzemmwIIXweIFs\SCrbjDh[pJq[2GwIHfy[YVvKG2xbnvlfUBEV1N5IHPlcIx{KGK7IH3pZ5Jwe2OxcHnjJHRmgGG|UnXkJIlu[WerbnesJGlEPTB;MUWg{txO M1LNZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNkKxOFc4Lz5{ME[yNVQ4PzxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CCND1 / CDK4 / p-JAK2 / JAK2 / p-STAT3 / STAT3 ; 

PubMed: 31534119     


The expression of CCND1, CDK4, p-JAK2, JAK2, p-STAT3, and STAT3 were detected by western blot after treated with dynasore for 0, 3, 6, 12, 24, and 48 h.

p-MET / MET ; 

PubMed: 29920310     


CAOV4 cells were serum-starved for 16hrs, followed by treatment with Dynasore at indicated concentrations for 30 mins. Cells were then stimulated with HGF for 30 mins, and the activation of MET was examined with pTyr1234/1235 MET antibody, with actin as loading control.

31534119 29920310
Immunofluorescence
STAT3 / p-STAT3 ; 

PubMed: 31534119     


The p-STAT3 and STAT3 expression were detected by using immunohistochemistry assay in MNNG/HOS (f) and MG-63 cells (g) (Scale bar: 20 μm). *p < 0.05 and **p < 0.01 vs. DMSO group.

31534119
Growth inhibition assay
Cell viability; 

PubMed: 31534119     


Cell viabilities of OS cells after treated with different concentrations of dynasore for 24, 48, and 72 h.

31534119

Protocol

Solubility (25°C)

In vitro DMSO 64 mg/mL (198.56 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
4mg/mL

* 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
in solvent
Synonyms N/A
Smiles C1=CC=C2C=C(C(=CC2=C1)C(=O)NN=CC3=CC(=C(C=C3)O)O)O

In vivo Formulation Calculator (Clear solution)

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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

Tel: +1-832-582-8158 Ext:3

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID