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
- Purity: > 99%
- Soluble in DMSO to 100 mM
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
Dynole® 34-2, dynamin I and dynamin II inhibitor -
Description
Potent dynamin I and dynamin II inhibitor -
Biological description
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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Purity
> 99% -
General notes
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 Number
1128165-88-7 -
Chemical structure
Properties
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Chemical name
2-Cyano-N-octyl-3-[1-(3-dimethylaminopropyl)-1H-indol-3-yl]acrylamide -
Molecular weight
408.59 -
Molecular formula
C25H36N4O -
PubChem identifier
44157463 -
Storage instructions
Store at +4°C. Store under desiccating conditions. The product can be stored for up to 12 months. -
Solubility overview
Soluble in DMSO to 100 mM -
Handling
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
CCCCCCCCNC(=O)C(C#N)=Cc2cn(CCCN(C)C)c1ccccc12 -
Source
Synthetic
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Research areas
Images
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Functional Studies - Dynole® 34-2, dynamin I and dynamin II inhibitor (ab120463)
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. -
Functional Studies - Dynole® 34-2, dynamin I and dynamin II inhibitor (ab120463) Image from Kockx et al., PLOS One., 9(10): e111186. Fig 1F.; doi: https://doi.org/10.1371/journal.pone.0111186. Reproduced under the Creative Commons license http://creativecommons.org/licenses/by/4.0/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.
