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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C18H14N2O4 |
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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) |
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* <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. |
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). |
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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] |
キナーゼアッセイ | GTPase activity assay | |
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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. |
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.]
Signaling via a CD27-TRAF2-SHP-1 axis during naive T cell activation promotes memory-associated gene regulatory networks [ Immunity, 2024, 57(2):287-302.e12] | PubMed: 38354704 |
Gonococcal OMV-delivered PorB induces epithelial cell mitophagy [ Nat Commun, 2024, 15(1):1669] | PubMed: 38396029 |
Repurposing a tricyclic antidepressant in tumor and metabolism disease treatment through fatty acid uptake inhibition [ J Exp Med, 2023, 220(3)e20221316] | PubMed: 36520461 |
SAMHD1-induced endosomal FAK signaling promotes human renal clear cell carcinoma metastasis by activating Rac1-mediated lamellipodia protrusion [ Exp Mol Med, 2023, 55(4):779-793] | PubMed: 37009792 |
RAGA prevents tumor immune evasion of LUAD by promoting CD47 lysosome degradation [ Commun Biol, 2023, 6(1):211] | PubMed: 36823443 |
Regulated dynamic subcellular GLUT4 localization revealed by proximal proteome mapping in human muscle cells [ J Cell Sci, 2023, 136(23)jcs261454] | PubMed: 38126809 |
Porcine deltacoronavirus enters ST cells by clathrin-mediated endocytosis and does not require Rab5, Rab7, or Rab11 [ Microbiol Spectr, 2023, 10.1128/spectrum.02553-23] | PubMed: 37962380 |
Low-dose metformin targets the lysosomal AMPK pathway through PEN2 [ Nature, 2022, 603(7899):159-165] | PubMed: 35197629 |
The aldolase inhibitor aldometanib mimics glucose starvation to activate lysosomal AMPK [ Nat Metab, 2022, 4-10:1369-1401] | PubMed: 36217034 |
α-Synuclein-containing erythrocytic extracellular vesicles: essential contributors to hyperactivation of monocytes in Parkinson's disease [ J Neuroinflammation, 2022, 19(1):53] | PubMed: 35193594 |
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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