Dyngo-4a

Alias:
Cat No.:V1592 Purity: ≥98%
Dyngo-4a (Dyngo 4a; Hydroxy Dynasore) is a potent and novel dynamin inhibitor with the potential to treatbotulism.
Dyngo-4a Chemical Structure CAS No.: 1256493-34-1
Product category: Dynamin
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Dyngo-4a (Dyngo 4a; Hydroxy Dynasore) is a potent and novel dynamin inhibitor with the potential to treat botulism. It inhibits dynamin 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Large GTPase dynein cleaves clathrin-coated vesicles that are membrane-bound. In cell physiology, endocytosis—the internalization of extracellular material and portions of the cytoplasmic membrane—is essential. With IC50 values of 2.7 μM and 0.38 μM, Hydroxy Dynasore inhibits dynamin I (Dyn I) activity in the GTPase assay [1], whether or not 0.06% Tween-80 is present. In U2OS cells, Hydroxy Dynasore inhibited Tfn-A594 uptake with an IC50 of 5.7 μM in clathrin-mediated endocytosis (CME) [1]. In the absence of Tween -80, Hydroxy Dynasore had IC50 values of 0.38 μM and 1.1 μM, while in the presence of Tween -80, IC50 values of 4.9 μM and 30.0 μM, respectively. Hydroxy Dynasore exhibits 2.1 times greater selectivity for DynI in this GTPase experiment compared to DynII of Sf21 cells and DynII (a recombinant protein derived from Sf21 cells) [1]. In motor nerve terminals and cultured hippocampus neurons, Hydroxy Dynasore inhibits the absorption of BoNT/A-Hc [2]. Hippocampal neurons depolarize when exposed to Hydroxy Dynasore (1-100 μM; 20 minutes before Alexa Fluor 488-BoNT/A-Hc addition); this inhibitory effect is dose-dependent and has an IC50 of 16.0 μM[2].
ln Vivo
In the phrenic nerve-diaphragm twitch model in CD-1 mice, Hydroxy Dynasore (ip; 30 mg/kg; 1.5–2 hours before BoNT/A injection) once more offered protection against BoNT/A-induced paralysis [2].
Animal Protocol
Animal/Disease Models: CD-1 mice[2].
Doses: 30 mg/kg
Route of Administration: intraperitoneal (ip)injection; 1.5–2 h before BoNT/A injection
Experimental Results: Protected BoNT/A-induced paralysis in vivo.
References
[1]. Adam McCluskey, et al. Building a Better Dynasore: The Dyngo Compounds Potently Inhibit Dynamin and Endocytosis. Traffic. 2013 Dec;14(12):1272-89.
[2]. Callista B Harper, et al.Dynamin Inhibition Blocks Botulinum Neurotoxin Type A Endocytosis in Neurons and Delays Botulism.J Biol Chem. 2011 Oct 14;286(41):35966-76.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H14N2O5
Molecular Weight
338.31
CAS #
1256493-34-1
SMILES
OC1=C(C(N/N=C/C2=CC(O)=C(O)C=C2O)=O)C=C3C=CC=CC3=C1
InChi Key
UAXHPUSKEWEOAP-DJKKODMXSA-N
InChi Code
InChI=1S/C18H14N2O5/c21-14-8-17(24)16(23)7-12(14)9-19-20-18(25)13-5-10-3-1-2-4-11(10)6-15(13)22/h1-9,21-24H,(H,20,25)/b19-9+
Chemical Name
3-Hydroxynaphthalene-2-carboxylic acid 2-[(2,4,5-trihydroxyphenyl)methylene]hydrazide
Synonyms

Dyngo-4a; Dyngo 4a; Hydroxy Dynasore; Dyngo4a;

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 67 mg/mL (198.0 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9559 mL 14.7793 mL 29.5587 mL
5 mM 0.5912 mL 2.9559 mL 5.9117 mL
10 mM 0.2956 mL 1.4779 mL 2.9559 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Dyngo-4a

    Dyngo compounds are potent, reversible inhibitors of endocytosis in non‐neuronal cells. Traffic. 2013 Dec;14(12):1272-89.
  • Dyngo-4a

    Dyngo compound 4a inhibits SVE in synaptosomes and neurons. Traffic. 2013 Dec;14(12):1272-89.
  • Dyngo-4a

    Dyngo compound 4a inhibits both CME and ADBE. Traffic. 2013 Dec;14(12):1272-89.
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