Molecular Formula | C18H14N2O5 |
Molar Mass | 338.31 |
Density | 1.45±0.1 g/cm3(Predicted) |
Solubility | DMSO: >10mg/mL |
Appearance | powder |
Color | faint yellow to dark yellow |
pKa | 8.28±0.40(Predicted) |
Storage Condition | 2-8°C |
In vitro study | 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. 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. 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. Hydroxy Dynasore prevents the uptake of BoNT/A-Hc in cultured hippocampal neurons and in motor nerve terminals. 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. |
In vivo study | 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. Animal Model: CD-1 mice. Dosage: 30 mg/kg Administration: Intraperitoneal injection; 1.5–2 h before BoNT/A injection Result: Protected BoNT/A-induced paralysis in vivo. |
Hazard Symbols | N - Dangerous for the environment |
Risk Codes | 50 - Very Toxic to aquatic organisms |
Safety Description | 61 - Avoid release to the environment. Refer to special instructions / safety data sheets. |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.956 ml | 14.779 ml | 29.559 ml |
5 mM | 0.591 ml | 2.956 ml | 5.912 ml |
10 mM | 0.296 ml | 1.478 ml | 2.956 ml |
5 mM | 0.059 ml | 0.296 ml | 0.591 ml |
biological activity | Hydroxy Dynasore (Dyngo-4a) is a structural analog of Dynasore (HY-15304), the low cytotoxic and universal dynamin inhibitors have IC50 values of 0.38 μm and 2.3 μm for brain recombinant dynamin I and recombinant murine dynamin II, respectively. Hydroxy Dynasore inhibits the endocytosis of dynamin-dependent transferrin with an IC50 of 5.7 μm. |
in vitro study | Dynamin is a large GTPase atmosphere. Endocytosis, internalizes portions of cells' plasma membrane along with extracellular material, is fundamentally important in cell physiology. Hydroxy Dynasore inhibitors 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. 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. 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. Hydroxy Dynasore prevents the uptake of BoNT/A-Hc in cultured hippocampal neurons and in motor nerve terminals. Hydroxy Dynasore (1-100μM; 20 min prior to 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. |
in vivo study | hydrodynasore (intraperone injection; 30 mg/kg; 1.5-2 h before BoNT/A injection) provide protection again BoNT/A-induced paralysis in the phonic nerve-hemidiaphragm twitch model in CD-1 mice. Animal Model: CD-1 mice. Dosage: 30 mg/kg Administration: intraperithonal injection; 1.5-2 h before BoNT/A injection Result: Protected BoNT/A-induced paralysis in vivo. |
Animal Model: | CD-1 mice. |
Dosage: | 30 mg/kg |
Administration: | Intraperitoneal injection; 1.5–2 h before BoNT/A injection |
Result: | Protected BoNT/A-induced paralysis in vivo. |