1. Cytoskeleton
  2. Dynamin
  3. Hydroxy-Dynasore

Hydroxy-Dynasore (Synonyms: Dyngo-4a)

Cat. No.: HY-13863
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Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.

For research use only. We do not sell to patients.

Hydroxy-Dynasore Chemical Structure

Hydroxy-Dynasore Chemical Structure

CAS No. : 1256493-34-1

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Description

Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.

In Vitro

Dynamin is a large GTPase enzyme that severs membrane‐bound clathrin‐coated vesicles. Endocytosis internalizes portions of cells’ plasma membrane along with extracellular material, is fundamentally important in cell physiology.
Hydroxy Dynasore inhibits Dynamin I (Dyn I) activity with IC50 values of 2.7 μM and 0.38 μM with or without 0.06% Tween‐80 in the GTPase assay[1].
Hydroxy Dynasore shows an IC50 of 5.7 μM in clathrin‐mediated endocytosis (CME) assay for inhibition of Tfn‐A594 uptake in U2OS cells[1].
Hydroxy Dynasore shows IC50 values of 0.38 μM and 1.1 μM in absence of Tween-80, and exhibits IC50 values of 4.9 μM and 30.0 μM in presence of Tween-80, respectively. Hydroxy Dynasore is 2.1‐fold selective for DynI versus DynII from Sf21 cells] and DynII (recombinant protein from Sf21 cells) in this GTPase assay[1].
Hydroxy Dynasore prevents the uptake of BoNT/A-Hc in cultured hippocampal neurons and in motor nerve terminals[2].
Hydroxy Dynasore (1-100μM; 20 min prior to the addition of Alexa Fluor 488-BoNT/A-Hc) results in depolarization of Hippocampal neurons, it dose-dependently inhibits internalization of Alexa Fluor 488-BoNT/A-Hc with an IC50 of 16.0 ± 1.2 μM[2].

In Vivo

Hydroxy Dynasore (intraperitoneal injection; 30 mg/kg; 1.5-2 h before BoNT/A injection) provides protection again BoNT/A-induced paralysis in the phrenic nerve-hemidiaphragm twitch model in CD-1 mice[2].

Animal Model: CD-1 mice[2].
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; 1.5–2 h before BoNT/A injection
Result: Protected BoNT/A-induced paralysis in vivo.
Molecular Weight

338.31

Formula

C₁₈H₁₄N₂O₅

CAS No.

1256493-34-1

SMILES

OC1=CC2=CC=CC=C2C=C1C(N/N=C/C3=C(O)C=C(O)C(O)=C3)=O

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Hydroxy-DynasoreDyngo-4aDynaminNeuronEndocytosis,Dynamin,GTPaseclathrin‐coatedvesicleInhibitorinhibitorinhibit

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