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    Dynasore
    Dynasore

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1590
    CAS #: 304448-55-3Purity ≥98%

    Description: Dynasore is a potent, cell-permeable, and reversible non-competitive dynamin inhibitor of GTPase activity of dynamin 1/2, with IC50 of 15 μM in a cell-free assay, it inhibits the mitochondrial dynamin Drp1 and has no effect against other small GTPase. Dynasore disrupts trafficking of herpes simplex virus proteins. It also enhances the formation of mitochondrial antiviral signalling aggregates and endocytosis-independent NF-κB activation. Dynasore protects mitochondria and improves cardiac lusitropy in Langendorff perfused mouse heart.

    References: Dev Cell. 2006 Jun;10(6):839-50; Dev Cell. 2006 Jun;10(6):839-50.

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    Molecular Weight (MW)322.31
    FormulaC18H14N2O4 
    CAS No.304448-55-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 64 mg/mL (198.6 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (E)-N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide

    InChi Key: SYNDQCRDGGCQRZ-VXLYETTFSA-N

    InChi Code: InChI=1S/C18H14N2O4/c21-15-6-5-11(7-17(15)23)10-19-20-18(24)14-8-12-3-1-2-4-13(12)9-16(14)22/h1-10,21-23H,(H,20,24)/b19-10+

    SMILES Code: OC1=CC2=CC=CC=C2C=C1C(N/N=C/C3=CC(O)=C(O)C=C3)=O           

    SynonymsDynasore


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    In Vitro

    In vitro activity: 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%. 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. 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.


    Cell Assay: Dynasore is a potent GTPases inhibitor and functions on the sites of dynamin1, dynamin2 or Drp1. When tested with HL-1 cells, treated cells with dynasore blocked the endocytic process via inhibiting the activity of dynamin.  Using genetically encoded pH-sensitive fluorescent probe synaptopHluorin to study the role of dynasore in the synapses expressing spH, and the results showed that dyansore treatment resulted in the normal stimulus-triggered increase in fluorescence intensity via reducing the GTPase activity of dynamin which in turn blocked the synaptic endocytosis. Dynasore worked as inhibitor of dynamin GTPase activity which blocks dynamin-dependent endocytosis not only in cells, but also including neurons.

    In VivoDynasore ameliorates the motor dysfunction greatly at 3, 7, and 10 days after SCI in rats. Dynasore significantly enhances motor function which may be by inhibiting the activation of neuronal mitochondrial apoptotic pathway and astrocytic proliferation in rats after SCI.
    Animal modelRats
    Formulation & DosageIn the dynasore groups, the rats are given dynasore immediately at a dose of 1, 10, or 30 mg/kg through intraperitoneal injection after SCI, while the rats in the sham and SCI groups receive DMSO (same volume as dynasore groups) through intraperitoneal injection
    References

    Dev Cell. 2006 Jun;10(6):839-50; Dev Cell. 2006 Jun;10(6):839-50.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Dynasore

    Dynasore reversibly blocks endocytosis in hippocampal synapses. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17955-60.
     

    Dynasore

    Dynasore has no immediate effect on exocytosis. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17955-60.
     

    Dynasore

    Endocytosis is blocked by dynasore during mild stimulation. Proc Natl Acad Sci U S A. 2006 Nov 21;103(47):17955-60.


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