product name Dyngo-4a
Description: Dyngo-4a is a potent, novel dynamin inhibitor with IC50 values of 0.38 μM, 1.1 μM, and 2.3 μM for DynI (brain), DynI (rec), and DynII (rec), respectively. Dyngo-4a (100 μM) caused a reduction in β-catenin levels in human colon carcinoma RKO cells. In addition, Dyngo-4a prevented the uptake of BoNT/A-Hc and blocked BoNT/A-induced SNAP25 cleavage in cultured hippocampal neurons.
References: Traffic. 2013 Dec;14(12):1272-89; J Cell Sci. 2014 Nov 15;127(Pt 22):4918-26.
338.31
Formula
C18H14N2O5
CAS No.
1256493-34-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 67 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19415334
| In Vitro |
In vitro activity: 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. In motor nerve terminals and cultured hippocampal neurons, Dyngo-4a blocks Alexa Fluor 488-BoNT/A-Hc internalization. In Drosophila S2R+ cells, Dyngo-4a causes a decrease in the level of Armadillo/β-catenin. Kinase Assay: Cell Assay: Dyngo-4a (100 μM) caused a reduction in β-catenin levels in human colon carcinoma RKO cells. In addition, Dyngo-4a prevented the uptake of BoNT/A-Hc and blocked BoNT/A-induced SNAP25 cleavage in cultured hippocampal neurons. Dyngo-4a is potent, reversible endocytosis inhibitor in non-neuronal cells. Dyngo-4a inhibited synaptic vesicle endocytosis (SVE) in synaptosomes and neurons with an IC50 value of 26.8 μM. |
|---|---|
| In Vivo | Dynamin is a potential therapeutic target for counteracting botulism. Dyngo-4a (30 mg/kg, intraperitoneal injection) treatment suppressed BoNT/A-induced muscle paralysis at the rat hemidiaphragm and significantly delayed the onset of botulism in an in vivo murine model. |
| Animal model | |
| Formulation & Dosage | |
| References | Traffic. 2013 Dec;14(12):1272-89; J Cell Sci. 2014 Nov 15;127(Pt 22):4918-26. |
