1256493-34-1
1256493-34-1 structure
- Name: 2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(2,4,5-trihydroxyphenyl)Methylene]hydrazide
- Chemical Name: Hydroxy-Dynasore
- CAS Number: 1256493-34-1
- Molecular Formula: C18H14N2O5
- Molecular Weight: 338.314
- Catalog: Signaling Pathways Cytoskeleton Dynamin
- Create Date: 2016-03-26 22:19:37
- Modify Date: 2024-01-02 16:06:58
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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.
| Name | Hydroxy-Dynasore |
|---|---|
| Synonyms |
3-Hydroxynaphthalene-2-carboxylic acid-(2,4,5-trihydroxybenzylidene)-hydrazide
3-Hydroxy-N'-[(E)-(2,4,5-trihydroxyphenyl)methylene]-2-naphthohydrazide Dynamin Inhibitor IV 2-Naphthalenecarboxylic acid, 3-hydroxy-, 2-[(1E)-(2,4,5-trihydroxyphenyl)methylene]hydrazide |
| 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. |
|---|---|
| Related Catalog | |
| 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. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Molecular Formula | C18H14N2O5 |
| Molecular Weight | 338.314 |
| Exact Mass | 338.090271 |
| PSA | 122.38000 |
| LogP | 5.12 |
| Index of Refraction | 1.683 |
| Storage condition | -20℃ |
