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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
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.
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].
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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].
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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. |
Molecular Formula |
C18H14N2O5
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Molecular Weight |
338.31
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CAS # |
1256493-34-1
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SMILES |
OC1=C(C(N/N=C/C2=CC(O)=C(O)C=C2O)=O)C=C3C=CC=CC3=C1
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InChi Key |
UAXHPUSKEWEOAP-DJKKODMXSA-N
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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+
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Chemical Name |
3-Hydroxynaphthalene-2-carboxylic acid 2-[(2,4,5-trihydroxyphenyl)methylene]hydrazide
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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.
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.