2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
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.
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].
Kinase Assay
Cell Assay
Animal Administration
References
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