Dyngo-4a

Dyngo-4a

Catalog Number:
L002371365APE
Mfr. No.:
APE-B5997
Price:
$236
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      • Overview
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          Background

          Target: DynI (brain); DynI (rec); DynII (rec)IC50: 0.38 μM; 1.1 μM; 2.3 μMDyngo-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 [1]. Dynamin is a large GTPase enzyme that severs as membrane-bound clathrin-coated vesicles [1]. In vitro: Dyngo-4a (100 μM) caused a reduction in β-catenin levels in human colon carcinoma RKO cells [2]. In addition, Dyngo-4a prevented the uptake of BoNT/A-Hc and blocked BoNT/A-induced SNAP25 cleavage in cultured hippocampal neurons [3]. 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 [1].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 [3].

          1. McCluskey A, Daniel JA, Hadzic G, Chau N, Clayton EL, Mariana A, et al. Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic. 2013;14(12):1272-89.
          2. Gagliardi M, Hernandez A, McGough IJ, Vincent JP. Inhibitors of endocytosis prevent Wnt/Wingless signalling by reducing the level of basal beta-catenin/Armadillo. J Cell Sci. 2014;127(Pt 22):4918-26.
          3. Harper CB, Martin S, Nguyen TH, Daniels SJ, Lavidis NA, Popoff MR, et al. Dynamin inhibition blocks botulinum neurotoxin type A endocytosis in neurons and delays botulism. J Biol Chem. 2011;286(41):35966-76.

      • Properties
        • Alternative Name
          (E)-3-hydroxy-N'-(2,4,5-trihydroxybenzylidene)-2-naphthohydrazide
          CAS Number
          1256493-34-1
          Molecular Formula
          C18H14N2O5
          Molecular Weight
          338.31
          Purity
          98.00%
          Solubility
          ≥33.8 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
          Storage
          Store at -20°C

          * For Research Use Only

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