Dynasore

Catalog No.S8047

For research use only.

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

CAS No. 304448-55-3

Selleck's Dynasore has been cited by 39 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 NVTQOG5FTnWwY4Tpc44h[XO|YYm= MnfQTY5pcWKrdHnvckBw\iC2cnHud4ZmenKrbjD1dJRic2ViaX6gZYZzcWOjbjDndoVmdiCvb37r[ZkhS0:VNzDj[YxteyCkeTDtbYNzd3Olb4DpZ{BV\Xijc2Ll[EBqdWGpaX7nMEBKSzVyPUG1JO69VQ>? Ml25QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4MkG0O|coRjJyNkKxOFc4RC:jPh?=
Assay
Methods Test Index PMID
Western blot p-MET / MET ; CCND1 / CDK4 / p-JAK2 / JAK2 / p-STAT3 / STAT3 29920310 31534119
Immunofluorescence STAT3 / p-STAT3 31534119
Growth inhibition assay Cell viability 31534119

Protocol (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 322.31
Formula

C18H14N2O4

CAS No. 304448-55-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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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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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