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AB120463

Dynole® 34-2, dynamin I and dynamin II inhibitor

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(15 Publications)

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.
3 Images
Immunocytochemistry/ Immunofluorescence - Dynole® 34-2, dynamin I and dynamin II inhibitor (AB120463)
  • ICC/IF

Unknown

Immunocytochemistry/ Immunofluorescence - 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)
  • FuncS

PubMed

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.

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/

Chemical Structure - Dynole® 34-2, dynamin I and dynamin II inhibitor (AB120463)
  • Chemical Structure

Lab

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

Key facts

CAS number

1128165-88-7

Purity

>99%

Form

Solid

form

Molecular weight

408.6 Da

Molecular formula

C<sub>2</sub><sub>5</sub>H<sub>3</sub><sub>6</sub>N<sub>4</sub>O

PubChem

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

Product details

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.

Properties and storage information

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

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

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.

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.

Product protocols

Publications (15)

Recent publications for all applications. Explore the full list and refine your search

Viruses 16: PubMed39205315

2024

Kinetic Landscape of Single Virus-like Particles Highlights the Efficacy of SARS-CoV-2 Internalization.

Applications

Unspecified application

Species

Unspecified reactive species

Aleksandar Atemin,Aneliya Ivanova,Wiley Peppel,Rumen Stamatov,Rodrigo Gallegos,Haley Durden,Sonya Uzunova,Michael D Vershinin,Saveez Saffarian,Stoyno S Stoynov

Frontiers in cell and developmental biology 12:1381357 PubMed39108837

2024

Enhanced secretion of promyogenic exosomes by quiescent muscle cells.

Applications

Unspecified application

Species

Unspecified reactive species

Prabhavathy Devan,Ananga Ghosh,Pallavi Rao T,Swasti Raychaudhuri,Harikrishna Adicherla,Himadri Devanshi,Pallavi Kshetrapal,Jyotsna Dhawan

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 177:116991 PubMed38906021

2024

Novel selective inhibitors of macropinocytosis-dependent growth in pancreatic ductal carcinoma.

Applications

Unspecified application

Species

Unspecified reactive species

Silvia Brambillasca,Maria Rosaria Cera,Adrian Andronache,Sumit Kumar Dey,Giovanni Fagá,Daniele Fancelli,Emanuela Frittoli,Maurizio Pasi,Michela Robusto,Mario Varasi,Giorgio Scita,Ciro Mercurio

Frontiers in cell and developmental biology 10:1075364 PubMed36605723

2022

Mapping of Tilapia Lake Virus entry pathways with inhibitors reveals dependence on dynamin activity and cholesterol but not endosomal acidification.

Applications

Unspecified application

Species

Unspecified reactive species

Reem Abu Rass,Japhette Esther Kembou-Ringert,Rachel Zamostiano,Avi Eldar,Marcelo Ehrlich,Eran Bacharach

Life (Basel, Switzerland) 11: PubMed34575026

2021

Dynamin Inhibitors Prevent the Establishment of the Cytomegalovirus Assembly Compartment in the Early Phase of Infection.

Applications

Unspecified application

Species

Unspecified reactive species

Igor Štimac,Natalia Jug Vučko,Gordana Blagojević Zagorac,Marina Marcelić,Hana Mahmutefendić Lučin,Pero Lučin

Tissue barriers 9:1929786 PubMed34107845

2021

Asymmetric distribution of dynamin-2 and β-catenin relative to tight junction spikes in alveolar epithelial cells.

Applications

Unspecified application

Species

Unspecified reactive species

K Sabrina Lynn,Kristen F Easley,Francisco J Martinez,Ryan C Reed,Barbara Schlingmann,Michael Koval

International immunopharmacology 84:106510 PubMed32361568

2020

ERK is involved in the differentiation and function of dimethyl sulfoxide-induced HL-60 neutrophil-like cells, which mimic inflammatory neutrophils.

Applications

Unspecified application

Species

Unspecified reactive species

Duo Wang,Yusuke Sennari,Mengyue Shen,Kentaro Morita,Tamotsu Kanazawa,Yasuhiro Yoshida

Cell reports 30:2444-2459.e7 PubMed32075774

2020

CtBP1-Mediated Membrane Fission Contributes to Effective Recycling of Synaptic Vesicles.

Applications

Unspecified application

Species

Unspecified reactive species

Daniela Ivanova,Cordelia Imig,Marcial Camacho,Annika Reinhold,Debarpan Guhathakurta,Carolina Montenegro-Venegas,Michael A Cousin,Eckart D Gundelfinger,Christian Rosenmund,Benjamin Cooper,Anna Fejtova

Science signaling 11: PubMed30065026

2018

Contact inhibitory Eph signaling suppresses EGF-promoted cell migration by decoupling EGFR activity from vesicular recycling.

Applications

Unspecified application

Species

Unspecified reactive species

Wayne Stallaert,Yannick Brüggemann,Ola Sabet,Lisa Baak,Marina Gattiglio,Philippe I H Bastiaens

Scientific reports 7:4580 PubMed28676641

2017

Dynamin-2 mutations linked to Centronuclear Myopathy impair actin-dependent trafficking in muscle cells.

Applications

Unspecified application

Species

Unspecified reactive species

Arlek M González-Jamett,Ximena Baez-Matus,María José Olivares,Fernando Hinostroza,Maria José Guerra-Fernández,Jacqueline Vasquez-Navarrete,Mai Thao Bui,Pascale Guicheney,Norma Beatriz Romero,Jorge A Bevilacqua,Marc Bitoun,Pablo Caviedes,Ana M Cárdenas
View all publications

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