[CAS NO. 1256493-34-1] Hydroxy-Dynasore
PRODUCTS SPECIFICATIONS [1256493-34-1]
DESCRIPTION [1256493-34-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 338.31 |
| Molecular Formula | C18H14N2O5 |
| SMILES | OC1=CC2=CC=CC=C2C=C1C(N/N=C/C3=C(O)C=C(O)C(O)=C3)=O |
1 Publications Citing Use of MCE
Summary
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC 50 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 IC 50 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 IC
50
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 IC
50
of 5.7 μM in clathrin‐mediated endocytosis (CME) assay for inhibition of Tfn‐A594 uptake in U2OS cells
[1]
.
Hydroxy Dynasore shows IC
50
values of 0.38 μM and 1.1 μM in absence of Tween-80, and exhibits IC
50
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 IC
50
of 16.0 ± 1.2 μM
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 184.74 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
-
1.
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.