Name | Dynasore |
Synonyms | DYNASORE Dynasore Dynasore monohydrate Dynasore monohydrate (E)-N'-(3,4-DIHYDROXYBENZYLIDENE)-3-HYDROXY-2-NAPHTHOHYDRAZIDE 3-Hydroxynaphthalene-2-carboxylicacid(3,4-dihydroxybenzylidene)hydrazide 3-Hydroxy-2-naphthalenecarboxylic acid [(3,4-dihydroxyphenyl)Methylene]hydrazide 2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(3,4-dihydroxyphenyl)methylene]hydrazide 3-Hydroxy-naphthalene-2-carboxylic acid (3,4-dihydroxy-benzylidene)-hydrazide monohydrate 3-Hydroxy-naphthalene-2-carboxylic acid (3,4-dihydroxy-benzylidene)-hydrazide monohydrate 3-Hydroxy-2-naphthalenecarboxylic acid [(3,4-dihydroxyphenyl)methylene]hydrazide Dynasore 3-hydroxy-N'-[(E)-(3-hydroxy-4-oxocyclohexa-2,5-dien-1-ylidene)methyl]naphthalene-2-carbohydrazide |
CAS | 304448-55-3 |
EINECS | 200-256-5 |
Molecular Formula | C18H14N2O4 |
Molar Mass | 322.31 |
Density | 1.36±0.1 g/cm3(Predicted) |
Melting Point | >224°C (dec.) |
Solubility | Soluble in DMSO (up to 30 mg/ml), or in Ethanol (up to 1 mg/ml). |
Appearance | Off-white solid. |
Color | Beige |
pKa | 8.49±0.35(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 month. |
Physical and Chemical Properties | Bioactive Dynasore is a cell-permeable, reversible, non-competitive dynamin inhibitor that inhibits GTPase activity of dynamin 1/2 with an IC50 of 15 μm in a cell-free assay, also inhibits mitochondrial dynamin Drp1 and has no effect on other small GTPases. Dynasore inhibits mTORC1 activity and induces autophagy. Dynasore inhibits multiple Virus of invasion, including HSV. |
Use | An inhibitor of Dynamin I and Dynamin II |
In vitro study | Dynaosre effectively inhibits the dynamin-dependent endocytosis pathway by rapidly inhibiting the formation of envelope vesicles within seconds of addition of Dynasore. During the Dynaosre treatment, two types of capsular caveolae intermediates accumulate, the U-form being a semi-formed capsular caveolae and the O-form being a fully formed capsular caveolae. 80 μm Dynasore also inhibited the enzymatic activity of mitochondrial dynamin Drp1. Dynaosre acts on HeLa cells and strongly inhibits the absorption, transport and intracellular accumulation of transferrin with an IC50 of 15 μm. Dynasore also inhibits endocytosis of low-density lipoproteins and Cholera toxin. Dynaosre (80 μm) strongly interfered with the spread of freshly seeded cells and inhibited BSC1 cell migration by 50%. Dynaosre completely and reversibly inhibited endocytosis after continuous or transient action potential stimulation in cultured hippocampal neurons, with complete inhibition at 80 μm and half-maximal inhibition of 30 μm. In the presence of Dynaosre, low-frequency stimulation leads to persistent accumulation of synaptophororin and other vesicular proteins on the surface membrane, at the rate predicted from net exocytosis, when the endocytic structure is only in the presence of synapses, reduces the density of synaptic vesicles. Dynasore inhibited infection of human epithelial cells HEK 293 with human papilloma Virus type 16 and bovine papilloma Virus type 1 to Virus with an equivalent IC50 of ~ 80 μm and was partially reversible. Dynaosre effectively inhibits the dynamin-dependent endocytosis pathway by rapidly inhibiting the formation of capsular vesicles within seconds of addition of Dynasore. During the Dynaosre treatment, two types of capsular caveolae intermediates accumulate, the U-form being a semi-formed capsular caveolae and the O-form being a fully formed capsular caveolae. 80 μm Dynasore also inhibited the enzymatic activity of mitochondrial dynamin Drp1. Dynaosre acts on HeLa cells and strongly inhibits the absorption, transport and intracellular accumulation of transferrin with an IC50 of 15 μm. Dynasore also inhibits endocytosis of low-density lipoproteins and Cholera toxin. Dynaosre (80 μm) strongly interfered with the spread of freshly seeded cells and inhibited BSC1 cell migration by 50%. Dynaosre completely and reversibly inhibited endocytosis after continuous or transient action potential stimulation in cultured hippocampal neurons, with complete inhibition at 80 μm and half-maximal inhibition of 30 μm. In the presence of Dynaosre, low-frequency stimulation leads to persistent accumulation of synaptophororin and other vesicular proteins on the surface membrane, at the rate predicted from net exocytosis, when the endocytic structure is only in the presence of synapses, reduces the density of synaptic vesicles. Dynasore inhibited infection of human epithelial cells HEK 293 with human papilloma Virus type 16 and bovine papilloma Virus type 1 to Virus with an equivalent IC50 of ~ 80 μm and was partially reversible. |
In vivo study | Dynasore 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. |
Hazard Symbols | N - Dangerous for the environment |
Risk Codes | 50 - Very Toxic to aquatic organisms |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
UN IDs | UN 3077 9/PG 3 |
Reference Show more | 1. [IF=11.413] Xiaojie Chen et al. |
Target
Target Value
Dynamin1/2
(Cell-free assay) ~15 μM
in vitro studies
Dynaosre effectively inhibited the dynamin-dependent endocytosis pathway by rapidly inhibiting the formation of capsular vesicles within seconds of addition of Dynasore. During Dynaosre treatment, two types of capsular fossa intermediates accumulate, the U-form being a semi-formed capsular fossa and the O-form being a fully formed capsular fossa. 80 μm Dynasore also inhibited the enzymatic activity of mitochondrial dynamin Drp1. Dynaosre acts on HeLa cells and strongly inhibits the absorption, transport and intracellular accumulation of transferrin with an IC50 of 15 μm. Dynasore also inhibits endocytosis of low-density lipoproteins and Cholera toxin. Dynaosre (80 μm) strongly interfered with the spread of freshly seeded cells and inhibited BSC1 cell migration by 50%. Dynaosre completely and reversibly inhibited endocytosis after continuous or transient action potential stimulation in cultured hippocampal neurons, with complete inhibition at 80 μm and half-maximal inhibition of 30 μm. In the presence of Dynaosre, low-frequency stimulation leads to persistent accumulation of synaptophororin and other vesicular proteins on the surface membrane, at the rate predicted from net exocytosis, when the endocytic structure is only in the presence of synapses, reduces the density of synaptic vesicles. Dynasore inhibited infection of human epithelial cells HEK 293 with human papilloma Virus type 16 and bovine papilloma Virus type 1 to Virus with an equivalent IC50 of ~ 80 μm and was partially reversible.
in vivo studies
Dynasore 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.
biological activity | Dynasore is a cell-permeable, reversible, non-competitive dynamin (engine protein) inhibitor that inhibits dynamin 1/2 of GTPase activity, IC50 is 15 μM, and also inhibits mitochondrial dynamin Drp1, it has no effect on other small GTPases. Dynasore is a cell-permeable, reversible, non-competitive dynamin inhibitor, which inhibits dynamin 1/2 of GTPase activity. IC50 is 15 μM in cell-free test, and also inhibits mitochondrial dynamin Drp1. It has no effect on other small GTPases. Dynasore can inhibit mTORC1 activity and induce autophagy. Dynasore inhibit the invasion of many viruses, including HSV. |
In vitro study | Dynaosre effectively inhibit the dynamin-dependent endocytosis pathway by rapidly inhibiting the formation of envelope vesicles within seconds of adding Dynasore. During the Dynaosre treatment, intermediates of the two types of coating cells accumulate, with U-shaped semi-formed coating cells and O-shaped fully formed coating cells. 80 μM Dynasore also inhibited the enzyme activity of mitochondrial dynamin Drp1. Dynaosre acts on HeLa cells and strongly inhibits the absorption, transport and intracellular accumulation of transferrin with an IC50 of 15 μM. Dynasore also inhibited the endocytosis of low-density lipoprotein and Cholera toxin. Dynaosre (80 μM) strongly interfered with the diffusion of fresh inoculated cells and inhibited the migration of 50% BSC1 cells. Dynaosre acts on cultured hippocampal neurons, and after continuous or transient action potential stimulation, completely and reversibly inhibits endocytosis. It is completely inhibited at 80 μM, and the semi-maximum inhibition is 30 μM. In the presence of Dynaosre, low-frequency stimulation leads to the continuous accumulation of synaptopHluorin and other vesicular proteins on the surface membrane. At the rate predicted from net exocytosis, when only synapses are present in endocytic structures, the density of synaptic vesicles is reduced. Dynasore inhibit human epithelial cell HEK 293 infection of human papillomavirus type 16 and bovine papillomavirus type 1 virus-like, the equivalent IC50 is ~ 80 μM, and is partially reversible. Dynaosre effectively inhibit the dynamin-dependent endocytosis pathway, and quickly inhibit the formation of envelope vesicles within a few seconds of adding Dynasore. During the Dynaosre treatment, intermediates of the two types of coating cells accumulate, with U-shaped semi-formed coating cells and O-shaped fully formed coating cells. 80 μM Dynasore also inhibited the enzyme activity of mitochondrial dynamin Drp1. Dynaosre acts on HeLa cells and strongly inhibits the absorption, transport and intracellular accumulation of transferrin with an IC50 of 15 μM. Dynasore also inhibited the endocytosis of low-density lipoprotein and Cholera toxin. Dynaosre (80 μM) strongly interfered with the diffusion of fresh inoculated cells and inhibited the migration of 50% BSC1 cells. Dynaosre acts on cultured hippocampal neurons, and after continuous or transient action potential stimulation, completely and reversibly inhibits endocytosis. It is completely inhibited at 80 μM, and the semi-maximum inhibition is 30 μM. In the presence of Dynaosre, low-frequency stimulation leads to the continuous accumulation of synaptopHluorin and other vesicular proteins on the surface membrane. At the rate predicted from net exocytosis, when only synapses are present in endocytic structures, the density of synaptic vesicles is reduced. Dynasore inhibit human epithelial cell HEK 293 infection of human papillomavirus type 16 and bovine papillomavirus type 1 virus-like, the equivalent IC50 is ~ 80 μM, and is partially reversible. |
target | TargetValue Dynamin1/2 (Cell-free say) ~ 15 μM |
Target | Value |
Dynamin1/2 (Cell-free assay) | ~ 15 μM |
in vivo research | Dynasore 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. |