Dynasore

製品コードS8047 バッチS804703

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₈H₁₄N₂O₄

分子量

322.31

CAS No.

304448-55-3

Solubility (25°C)*

体外

DMSO

64 mg/mL (198.56 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 30%PEG300 2 5%Tween80 3 60%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.000mg/ml (12.41mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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).
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 its addition. Two types of coated pit intermediates accumulate during this compound's treatment, U-shaped, half formed pits and O-shaped, fully formed pits, captured while pinching off. This chemical at concentration of 80 μM, also inhibits the enzymatic activity of the mitochondrial dynamin Drp1. It strongly blocks the uptake, trafficking, and intracellular accumulation of transferrin in HeLa cells with IC50 of ~15 μM. It also prevents the endocytosis of low-density lipoprotein and cholera toxin. This compound (80 μM) strongly interferes with the spread of freshly plated cells, and inhibits BSC1 cells migration by about 50%. ^[1] It 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 this inhibitor, 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] It 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]

製品説明

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).

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 its addition. Two types of coated pit intermediates accumulate during this compound's treatment, U-shaped, half formed pits and O-shaped, fully formed pits, captured while pinching off. This chemical at concentration of 80 μM, also inhibits the enzymatic activity of the mitochondrial dynamin Drp1. It strongly blocks the uptake, trafficking, and intracellular accumulation of transferrin in HeLa cells with IC50 of ~15 μM. It also prevents the endocytosis of low-density lipoprotein and cholera toxin. This compound (80 μM) strongly interferes with the spread of freshly plated cells, and inhibits BSC1 cells migration by about 50%. ^[1]

It 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 this inhibitor, 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]

It 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]

プロトコル(参考用のみ)

キナーゼアッセイ	GTPase activity assay
キナーゼアッセイ	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.
細胞アッセイ	細胞株	Cell-free assays
	濃度	15 µM
	反応時間
	実験の流れ
動物実験	動物モデル	Female Sprague–Dawley rats
	投薬量	1, 10, or 30 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/16740485/
https://pubmed.ncbi.nlm.nih.gov/17093049/
https://pubmed.ncbi.nlm.nih.gov/18645330/

https://pubmed.ncbi.nlm.nih.gov/27822712/

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カスタマーフィードバック

: 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.]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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