Dyngo-4a

製品コードS7163 バッチS716301

印刷

化学情報

Chemical Structure Synonyms Hydroxy-Dynasore Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H14N2O5
分子量 338.31 CAS No. 1256493-34-1
Solubility (25°C)* 体外 DMSO 67 mg/mL (198.04 mM)
Ethanol (warmed with 50ºC water bath) 1 mg/mL (2.95 mM)
Water 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.
* <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 Dyngo-4a is a potent dynamin inhibitor with IC50 of 0.38 μM, 1.1 μM, and 2.3 μM for DynI (brain), DynI (rec), and DynII (rec), respectively.
in vitro Dyngo-4a inhibits dynamin-dependent endocytosis of transferrin in multiple cell types with IC₅₀ of 5.7 μM, and reduces synaptic vesicle endocytosis and activity-dependent bulk endocytosis in cultured neurons and synaptosomes. [1] In motor nerve terminals and cultured hippocampal neurons, this compound blocks Alexa Fluor 488-BoNT/A-Hc internalization. [2] In Drosophila S2R+ cells, it causes a decrease in the level of Armadillo/β-catenin. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Dynamin GTPase assay
Dynamin I activity is measured in its SAI activity state or is stimulated by three different methods. As each stimulus activates dynamin to different extents, each assay requires different dynamin concentrations. First, maximal dynamin activity is stimulated by sonicated PS liposomes. Purified dynamin I (10–20 nM, diluted in: 6 mM Tris–HCl, 20 mM NaCl and 0.01% Tween 80, pH 7.4) is incubated in 96-well plates in GTPase buffer (5 mM Tris–HCl, 10 mM NaCl, 2 mM Mg2+, 0.05% Tween 80, pH 7.4, 1 µg/mL leupeptin and 0.1 mM PMSF) and GTP 0.3 mM in the presence of test compound for 30 min at 37°C in a final assay volume of 150 μL. Reactions are terminated with 10 μL of 0.5 M ethylenediaminetetraacetic acid (EDTA) pH 7.4 and Malachite Green solution (40 μL: 2% w/v ammonium molybdate tetrahydrate, 0.15% w/v malachite green and 4 M HCl) is added for 5 min. Second, dynamin (20 nM) is stimulated by 10 µg/mL of taxol-stabilized preformed bovine brain microtubules using the same protocol. Third, dynamin I (50 nM) is stimulated by 1 μM of recombinant grb2, a SH3-containing protein that stimulates dynamin about 5–10 times less efficiently than liposomes or microtubules. Finally, dynamin (500 nM) SAI activity is measured using high concentrations of dynamin, which promote its cooperative self-assembly into rings (but not helices). The final DMSO concentration in the GTPase or endocytosis assays is at most 3.3 or 1%, respectively, but typically is at 1%. The GTPase assay for dynamin I is unaffected by DMSO up to 3.3%. Compounds are dissolved as 30 mM stocks in 100% DMSO. These stock solutions can be stored at −20°C for several months. Compounds are subsequently diluted into solutions of 50% DMSO made up in 20 mM Tris–HCl pH 7.4 and diluted again into the final assay. For analysis of the kinetics of this compound inhibition, dynamin I at a final concentration of 17 nM is incubated with GTPase buffer containing PS (2 µg/mL) and varying amounts of GTP (50–250 μM) in the presence of this chemical at a concentration range between 0.5 and 6 μM. The reaction is stopped after 30 min by addition of EDTA (0.5 mM, pH 7.4). Curves are generated using the Michaelis–Menten equation v = Vmax[S]/(Km + [S]), where S is the GTP substrate. After the Vmax and Km values were determined, the data were transformed using the Lineweaver–Burke equation, 1/v = 1/Vmax + (Km/Vmax)(1/[S]). Assay conditions are based on the dynamin I assay but contained modifications. Recombinant dynamin II is used at 50 nM, stimulated by 10 µg/mL PS. The GTPase reaction is allowed to occur for 90 min at 37°C before termination.
細胞アッセイ 細胞株 αT3–1 or LβT2 cells
濃度 30 μM
反応時間 30 minutes
実験の流れ

αT3-1 or LβT2 cells (2 × 106) were grown overnight in a 6-well culture dish and then serum starved for 2–4 hours. Cells were pretreated with either vehicle (0), dynasore (80μM), or dyngo (30μM) for 30 minutes. For dose-response studies, indicated doses of this compound were used for a 30-minute pretreatment. After pretreatment, cells were treated with 0 or GnRHa (10 nM) for 10 minutes. Cells were then washed twice in PBS, lysed in radio-immunoprecipitation assay (RIPA) buffer and subjected to SDS-PAGE (acrylamide:bis-acrylamide ratio of 29:1) and electroblotted to polyvinylidene difluoride membranes.
動物実験 動物モデル Female CD-1 mice
投薬量 30 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/24025110/
  • https://pubmed.ncbi.nlm.nih.gov/21832053/
  • https://pubmed.ncbi.nlm.nih.gov/25236598/
  • https://pubmed.ncbi.nlm.nih.gov/21832053/
  • https://pubmed.ncbi.nlm.nih.gov/26696122/

カスタマーフィードバック

Data from [Data independently produced by , , Cell Commun Signal, 2018, 16(1):40]

Data from [Data independently produced by , , J Immunol, 2018, 200(3):997-1007]

Data from [Data independently produced by , , Int J Biochem Cell Biol, 2018, 105:1-12]

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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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