Dynole® 34-2, dynamin I and dynamin II inhibitor (ab120463)
Key features and details
- Potent dynamin I and dynamin II inhibitor
- CAS Number: 1128165-88-7
- Soluble in DMSO to 100 mM
- Form / State: Solid
- Source: Synthetic
製品の概要
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製品名
Dynole® 34-2, dynamin I and dynamin II inhibitor -
製品の詳細
Potent dynamin I and dynamin II inhibitor -
生理活性の詳細
Potent, cell-permeable dynamin I and dynamin II inhibitor (IC50 values are 1.3 and 14.2 μM for inhibition of dynamin I and II GTPase, respectively). Targets the GTPase domain at an allosteric site. Potently inhibits receptor-mediated and synaptic vesicle endocytosis (IC50 values are 5 and 41.1 μM, respectively). 15-fold more active than Dynasore (ab120192) against dynamin I.
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特記事項
Sold under exclusive licence from Children's Medical Research Institute and Newcastle Innovation Ltd. Dynole® is a trademark of Children's Medical Research Institute and Newcastle Innovation Ltd. -
CAS 番号
1128165-88-7 -
構造式
製品の特性
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体系名
2-Cyano-N-octyl-3-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]acrylamide -
分子量
408.59 -
分子式
C25H36N4O -
PubChem 登録番号
44157463 -
保存方法
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
溶解性
Soluble in DMSO to 100 mM -
使用に関する注意
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES 線形表記
CCCCCCCCNC(=O)C(C#N)=Cc2cn(CCCN(C)C)c1ccccc12 -
由来
Synthetic
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研究分野
アプリケーション
The Abpromise guarantee
Abpromise保証は、 次のテスト済みアプリケーションにおけるab120463の使用に適用されます
アプリケーションノートには、推奨の開始希釈率がありますが、適切な希釈率につきましてはご検討ください。
アプリケーション | Abreviews | 特記事項 |
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Functional Studies |
Use at an assay dependent concentration.
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特記事項 |
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Functional Studies
Use at an assay dependent concentration. |
画像
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2D chemical structure image of ab120463, Dynole® 34-2, dynamin I and dynamin II inhibitor
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ab66705 staining PAI1 in HeLa cells treated with dynole-34-2™; (ab120463), by ICC/IF. Increase in PAI1 expression correlates with increased concentration of dynole-34-2™, as described in literature.
The cells were incubated at 37°C for 24h in media containing different concentrations of ab120463 (dynole-34-2™) in DMSO, fixed with 100% methanol for 5 minutes at -20°C and blocked with PBS containing 10% goat serum, 0.3 M glycine, 1% BSA and 0.1% tween for 2h at room temperature. Staining of the treated cells with ab66705 (5 µg/ml) was performed overnight at 4°C in PBS containing 1% BSA and 0.1% tween. A DyLight 488 goat anti-rabbit polyclonal antibody (ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue. -
Primary human monocyte-derived macrophages (HMDM) were incubated with 30 µM of ab120463 for indicated time periods to determine if Dynamin inhibition decreases apoE secretion from primary human macrophages. Dynole-34-2 both dose- and time-dependently decreased apoE secretion without affecting HMDM viability (botton line on the graph as appose to the control, top line).
Kockx et al., PLOS One., 9(10): e111186. Fig 1F.; doi: https://doi.org/10.1371/journal.pone.0111186.
プロトコール
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
参考文献 (12)
ab120463 は 12 報の論文で使用されています。
- Abu Rass R et al. Mapping of Tilapia Lake Virus entry pathways with inhibitors reveals dependence on dynamin activity and cholesterol but not endosomal acidification. Front Cell Dev Biol 10:1075364 (2022). PubMed: 36605723
- Lynn KS et al. Asymmetric distribution of dynamin-2 and ß-catenin relative to tight junction spikes in alveolar epithelial cells. Tissue Barriers N/A:1929786 (2021). PubMed: 34107845
- Štimac I et al. Dynamin Inhibitors Prevent the Establishment of the Cytomegalovirus Assembly Compartment in the Early Phase of Infection. Life (Basel) 11:N/A (2021). PubMed: 34575026
- Ivanova D et al. CtBP1-Mediated Membrane Fission Contributes to Effective Recycling of Synaptic Vesicles. Cell Rep 30:2444-2459.e7 (2020). PubMed: 32075774
- Wang D et al. ERK is involved in the differentiation and function of dimethyl sulfoxide-induced HL-60 neutrophil-like cells, which mimic inflammatory neutrophils. Int Immunopharmacol 84:106510 (2020). PubMed: 32361568