Dyngo-4a

Cas No.:	1256493-34-1
Chemical Name:	(E)-N'-(2,4,5-trihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide
SMILES:	OC1=CC2=CC=CC=C2C=C1C(N/N=C/C3=C(O)C=C(O)C(O)=C3)=O
Formula:	C18H14N2O5
M.Wt:	338.31
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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 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].