MW 408.6 Da, Purity >99%. 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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- Frontiers in cell and developmental biology 10:10753642022Mapping of Tilapia Lake Virus entry pathways with inhibitors reveals dependence on dynamin activity and cholesterol but not endosomal acidification.Applications:Unspecified applicationReactive species:Unspecified reactive speciesReem Abu Rass,Japhette Esther Kembou-Ringert,Rachel Zamostiano,Avi Eldar,Marcelo Ehrlich,Eran BacharachPubMed 36605723
- Life (Basel, Switzerland) 11:2021Dynamin Inhibitors Prevent the Establishment of the Cytomegalovirus Assembly Compartment in the Early Phase of Infection.Applications:Unspecified applicationReactive species:Unspecified reactive speciesIgor Štimac,Natalia Jug Vučko,Gordana Blagojević Zagorac,Marina Marcelić,Hana Mahmutefendić Lučin,Pero LučinPubMed 34575026
- Tissue barriers 9:19297862021Asymmetric distribution of dynamin-2 and β-catenin relative to tight junction spikes in alveolar epithelial cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesK Sabrina Lynn,Kristen F Easley,Francisco J Martinez,Ryan C Reed,Barbara Schlingmann,Michael KovalPubMed 34107845
- International immunopharmacology 84:1065102020ERK is involved in the differentiation and function of dimethyl sulfoxide-induced HL-60 neutrophil-like cells, which mimic inflammatory neutrophils.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDuo Wang et. al.PubMed 32361568
- Cell reports 30:2444-2459.e72020CtBP1-Mediated Membrane Fission Contributes to Effective Recycling of Synaptic Vesicles.Applications:Unspecified applicationReactive species:Unspecified reactive speciesDaniela Ivanova,Cordelia Imig,Marcial Camacho,Annika Reinhold,Debarpan Guhathakurta,Carolina Montenegro-Venegas,Michael A Cousin,Eckart D Gundelfinger,Christian Rosenmund,Benjamin Cooper,Anna FejtovaPubMed 32075774
- Science signaling 11:2018Contact inhibitory Eph signaling suppresses EGF-promoted cell migration by decoupling EGFR activity from vesicular recycling.Applications:Unspecified applicationReactive species:Unspecified reactive speciesWayne Stallaert et. al.PubMed 30065026
- Scientific reports 7:45802017Dynamin-2 mutations linked to Centronuclear Myopathy impair actin-dependent trafficking in muscle cells.Applications:Unspecified applicationReactive species:Unspecified reactive speciesArlek M González-Jamett et. al.PubMed 28676641
- PloS one 12:e01724432017Dynamin2 controls Rap1 activation and integrin clustering in human T lymphocyte adhesion.Applications:Unspecified applicationReactive species:Unspecified reactive speciesFelix J Eppler et. al.PubMed 28273099
- Cellular signalling 28:160-712015Impaired dynamin 2 function leads to increased AP-1 transcriptional activity through the JNK/c-Jun pathway.Applications:Unspecified applicationReactive species:Unspecified reactive speciesEwelina Szymanska,Agnieszka Skowronek,Marta MiaczynskaPubMed 26475677
Key facts
- CAS number
- 1128165-88-7
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 408.6 Da
- Molecular formula
- C25H36N4O
- PubChem identifier
- 44157463
- Nature
- Synthetic
Target data
Alternative names
B dynamin, CMT2M, CMTDI1, CMTDIB, DI CMTB, DNM, DNM 1, DYN II, DYN1_HUMAN, DYN2_HUMAN, Dynamin, Dynamin II, Dynamin-1, Dynamin-2
Recommended products
MW 408.6 Da, Purity >99%. 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.
Key facts
- CAS number
- 1128165-88-7
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 408.6 Da
- Molecular formula
- C25H36N4O
- PubChem identifier
- 44157463
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- Dynole 34-2
- 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.
- Canonical SMILES
- CCCCCCCCNC(=O)C(=CC1=CN(C2=CC=CC=C21)CCCN(C)C)C#N
- Isomeric SMILES
- CCCCCCCCNC(=O)/C(=C/C1=CN(C2=CC=CC=C21)CCCN(C)C)/C#N
- InChI
- InChI=1S/C25H36N4O/c1-4-5-6-7-8-11-15-27-25(30)21(19-26)18-22-20-29(17-12-16-28(2)3)24-14-10-9-13-23(22)24/h9-10,13-14,18,20H,4-8,11-12,15-17H2,1-3H3,(H,27,30)/b21-18+
- InChIKey
- MYIMRONQBLZJFI-DYTRJAOYSA-N
- IUPAC name
- (E)-2-cyano-3-[1-[3-(dimethylamino)propyl]indol-3-yl]-N-octylprop-2-enamide
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- +4°C
- Appropriate long-term storage conditions
- +4°C
- Storage information
- Store under desiccating conditions, The product can be stored for up to 12 months
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.
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Dynamin 1 and Dynamin 2 are important proteins playing an important mechanical role in cellular processes. Dynamin proteins are large with masses of about 96 kDa for Dynamin 1 and 100 kDa for Dynamin 2. They function as GTPases driving membrane constriction and fission. These processes help in membrane trafficking such as endocytosis. Both types of Dynamin are present in various tissues with Dynamin 1 being expressed mainly in the brain and neurons while Dynamin 2 is expressed in non-neuronal cells.
- Biological function summary
Dynamins are involved in essential tasks within cells specifically mediating membrane scission. Dynamin 1 along with Dynamin 2 forms helical structures around the neck of budding vesicles contributing to their detachment from the plasma membrane. These proteins work closely with actin and microtubule networks ensuring proper cytoskeleton-dependent trafficking. Dynamins can also interact with a complex of proteins including amphiphysin and endophilin enhancing their function.
- Pathways
Dynamins play significant roles in synaptic vesicle recycling and receptor-mediated endocytosis. These pathways are important for neurotransmitter release and nutrient uptake. In these contexts Dynamins interact with proteins like clathrin and sorting nexin. The GTPase activity of Dynamins is fundamental to their action in these pathways facilitating vesicle budding and fusion events.
- Associated diseases and disorders
Disruptions in Dynamin function are linked to cancer and neurological diseases. Mutations in Dynamin 2 can cause Charcot-Marie-Tooth disease a hereditary neuropathy affecting peripheral nerves. Additionally altered expression or function of Dynamins relates to cancer types like glioblastoma often through interactions with proteins such as EGFR which can exacerbate tumor progression and chemoresistance.
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3 product images
Chemical Structure - Dynole® 34-2, dynamin I and dynamin II inhibitor (ab120463)
2D chemical structure image of ab120463, Dynole® 34-2, dynamin I and dynamin II inhibitor
Immunocytochemistry/ Immunofluorescence - Dynole® 34-2, dynamin I and dynamin II inhibitor (ab120463)
Anti-PAI1 antibody 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 Anti-PAI1 antibody 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 (Goat Anti-Rabbit IgG H&L (DyLight® 488) preadsorbed ab96899) at 1/250 dilution was used as the secondary antibody. Nuclei were counterstained with DAPI and are shown in blue.
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/Functional Studies - Dynole® 34-2, dynamin I and dynamin II inhibitor (ab120463)
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.
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