For research use only. Not for therapeutic Use.
<p style=/line-height:25px/>Dynasore is a cell-permeable small molecule that inhibits the GTPase activity of dynamin1, dynamin2 and Drp1, the mitochondrial dynamin.<br>IC50 Value: 15 uM [1]<br>Target: dynamin<br>Dynasore was discovered in a screen of approximately 16,000 compounds for inhibitors of the dynamin2 GTPase. Dynasore is a noncompetitive inhibitor of dynamin GTPase activity and blocks dynamin-dependent endocytosis in cells, including neurons[2].<br>in vitro: Dynasore inhibits dynamin GTPase activity and transferrin uptake at IC(50) approximately 15 microM but use in some biological applications requires more potent inhibitor than dynasore. Dynasore treatment led to the abnormal accumulation of LDL and free cholesterol (FC) within the endolysosomal network. The measure of cholesterol esters (CE) further showed that the delivery of regulatory cholesterol to the endoplasmic reticulum (ER) was deficient. This resulted in the inhibition of the transcriptional control of the three major sterol-sensitive genes, sterol-regulatory element binding protein 2 (SREBP-2), 3-hydroxy-3-methyl-coenzymeA reductase (HMGCoAR), and low-density lipoprotein receptor (LDLR)[3].<br>in vivo:<br></p>
| Catalog Number | I003065 |
| CAS Number | 304448-55-3 |
| Synonyms | (E)-N/’-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide |
| Molecular Formula | C₁₈H₁₄N₂O₄ . H₂O |
| Purity | ≥95% |
| Target | ATPase |
| Solubility | 10 mM in DMSO |
| Storage | 3 years -20C powder |
| IC50 | 15 uM [1] |
| InChI | InChI=1S/C18H14N2O4/c21-15-6-5-11(7-17(15)23)10-19-20-18(24)14-8-12-3-1-2-4-13(12)9-16(14)22/h1-10,19,22-23H,(H,20,24)/b11-10+ |
| InChIKey | NRQJUIHYFNUXFT-ZHACJKMWSA-N |
| SMILES | C1=CC=C2C=C(C(=CC2=C1)C(=O)NNC=C3C=CC(=O)C(=C3)O)O |
| Reference | </br>1:Dynasore blocks evoked release while augmenting spontaneous synaptic transmission from primary visceral afferents. Hofmann ME, Andresen MC.PLoS One. 2017 Mar 30;12(3):e0174915. doi: 10.1371/journal.pone.0174915. eCollection 2017. PMID: 28358887 Free PMC Article</br>2:Dynasore impairs VEGFR2 signalling in an endocytosis-independent manner. Basagiannis D, Zografou S, Galanopoulou K, Christoforidis S.Sci Rep. 2017 Mar 22;7:45035. doi: 10.1038/srep45035. PMID: 28327657 Free PMC Article</br>3:Dynasore Improves Motor Function Recovery via Inhibition of Neuronal Apoptosis and Astrocytic Proliferation after Spinal Cord Injury in Rats. Li G, Shen F, Fan Z, Wang Y, Kong X, Yu D, Zhi X, Lv G, Cao Y.Mol Neurobiol. 2016 Nov 7. [Epub ahead of print] PMID: 27822712 </br>4:The dynamin inhibitor dynasore inhibits bone resorption by rapidly disrupting actin rings of osteoclasts. Thirukonda GJ, Uehara S, Nakayama T, Yamashita T, Nakamura Y, Mizoguchi T, Takahashi N, Yagami K, Udagawa N, Kobayashi Y.J Bone Miner Metab. 2016 Jul;34(4):395-405. doi: 10.1007/s00774-015-0683-1. Epub 2015 Jun 11. PMID: 26063501 </br>5:Dynasore – not just a dynamin inhibitor. Preta G, Cronin JG, Sheldon IM.Cell Commun Signal. 2015 Apr 10;13:24. doi: 10.1186/s12964-015-0102-1. Review. PMID: 25889964 Free PMC Article</br>6:Dynasore disrupts trafficking of herpes simplex virus proteins. Mues MB, Cheshenko N, Wilson DW, Gunther-Cummins L, Herold BC.J Virol. 2015 Jul;89(13):6673-84. doi: 10.1128/JVI.00636-15. Epub 2015 Apr 15. PMID: 25878109 Free PMC Article</br>7:Dynasore enhances the formation of mitochondrial antiviral signalling aggregates and endocytosis-independent NF-κB activation. Ailenberg M, Di Ciano-Oliveira C, Szaszi K, Dan Q, Rozycki M, Kapus A, Rotstein OD.Br J Pharmacol. 2015 Aug;172(15):3748-63. doi: 10.1111/bph.13162. Epub 2015 May 15. PMID: 25850711 Free PMC Article</br>8:The effect of dynasore, a blocker of dynamin-dependent endocytosis, on spontaneous quantal and non-quantal release of acetylcholine in murine neuromuscular junctions. Malomouzh AI, Mukhitov AR, Proskurina SE, Vyskocil F, Nikolsky EE.Dokl Biol Sci. 2014 Nov;459:330-3. doi: 10.1134/S0012496614060052. Epub 2015 Jan 6. No abstract available. PMID: 25560208 </br>9:Protective role of the dynamin inhibitor Dynasore against the cholesterol-dependent cytolysin of Trueperella pyogenes. Preta G, Lotti V, Cronin JG, Sheldon IM.FASEB J. 2015 Apr;29(4):1516-28. doi: 10.1096/fj.14-265207. Epub 2014 Dec 30. PMID: 25550455 Free PMC Article</br>10:The Dynamin 2 inhibitor Dynasore affects the actin filament distribution during mouse early embryo development. Wang QC, Liu J, Duan X, Cui XS, Kim NH, Xiong B, Sun SC.J Reprod Dev. 2015;61(1):49-53. doi: 10.1262/jrd.2014-079. Epub 2014 Nov 21. PMID: 25421092 Free PMC Article |
