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Submit ReviewDynasore is a non-competitive reversible inhibitor of dynamin 1, dynamin 2 and mitochondrial dynamin (Drp1) GTPase activity. Dynasore blocks endocytic pathways dependent on dynamin and inhibits cell spreading and migration of BSC1 cells. Dynasore attenuates motor symptoms in an animal model of Parkinson's disease and in a cellular model of Alzheimer's disease it reduces tau protein aggregation and internalization.
分子量 | 322.32 |
公式 | C18H14N2O4 |
储存 | Store at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 304448-55-3 |
PubChem ID | 5717066 |
InChI Key | NRQJUIHYFNUXFT-ZHACJKMWSA-N |
Smiles | O=C(N/N=C/C3=CC(O)=C(O)C=C3)C2=CC1=CC=CC=C1C=C2O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 32.23 | 100 |
以下数据基于产品分子量 322.32。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 3.1 mL | 15.51 mL | 31.03 mL |
5 mM | 0.62 mL | 3.1 mL | 6.21 mL |
10 mM | 0.31 mL | 1.55 mL | 3.1 mL |
50 mM | 0.06 mL | 0.31 mL | 0.62 mL |
参考文献是支持产品生物活性的出版物。
Thompson and McNiven (2006) Discovery of a new 'dynasore'. Nat.Chem.Biol. 2 355 PMID: 16783339
Macia et al (2006) Dynasore, a cell-permeable inhibitor of Dynamin. Develop.Cell 10 839
Newton et al (2006) Inhibition of dynamin completely blocks compensatory synaptic vesicle endocytosis. Proc.Natl.Acad.Sci.USA 103 17955
Feng et al (2021) Inhibition of dynamin-related protein 1 ameliorates the mitochondrial ultrastructure via PINK1 and Parkin in the mice model of Parkinson's disease. Eur.J.Pharmacol. 907 174262 PMID: 34146589
Soares et al (2021) PIKfyve activity is required for lysosomal trafficking of tau aggregates and tau seeding. J.Biol.Chem. 296 PMID: 33831417
If you know of a relevant reference for Dynasore, please let us know.
关键词: Dynasore, Dynasore supplier, Non-competitive, dynamin, 1, 2, mitochondrial, Drp1, inhibitors, inhibits, Mitosis, GTPases, Dynamin, 2897, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Dynasore 的部分引用包括:
Blume et al (2016) Cannabinoid receptor interacting protein suppresses agonist-driven CB1 receptor internalization and regulates receptor replenishment in an agonist-biased manner. J.Neurochem. 139 396 PMID: 27513693
Hallstrom and McCormick (2016) The type three secreted effector SipC regulates the trafficking of PERP during Salmonella infection. Gut Microbes 7 136 PMID: 27078059
Niederst et al (2015) Axonal amyloid precursor protein and its fragments undergo somatodendritic endocytosis and processing. Front Immunol 26 205 PMID: 25392299
Hoven et al (2015) eIF2α Confers Cellular Tolerance to S. aureus α-Toxin. Proc Natl Acad Sci U S A 6 383 PMID: 26284068
Park et al (2011) A selective inhibitor of drp1, mdivi-1, increases retinal ganglion cell survival in acute ischemic mouse retina. J Neurosci 52 2837 PMID: 21372007
Lussier et al (2011) Activity-dependent ubiquitination of the AMPA receptor subunit GluA2. Proc Natl Acad Sci U S A 31 3077 PMID: 21414928
Lorenz-Guertin et al (2017) A versatile optical tool for studying synaptic GABAA receptor trafficking. J Cell Sci 130 3933 PMID: 29025969
Ledonne et al (2015) Neuregulin 1 signalling modulates mGluR1 function in mesencephalic dopaminergic neurons. Mol Psychiatry 20 959 PMID: 25266126
Nimlamool et al (2015) Connexin43 phosphorylation by PKC and MAPK signals VEGF-mediated gap junction internalization. Mol Biol Cell 26 2755 PMID: 26063728
Lee et al (2014) Synergy between Piezo1 and Piezo2 channels confers high-strain mechanosensitivity to articular cartilage. J Neurosci 111 E5114 PMID: 25385580
Rodriguez et al (2011) Lethal iron deprivation induced by non-neutralizing antibodies targeting transferrin receptor 1 in malignant B cells. Leuk Lymphoma 52 2169 PMID: 21870996
Zemskov et al (2011) Unconventional secretion of tissue transglutaminase involves phospholipid-dependent delivery into recycling endosomes. PLoS One 6 e19414 PMID: 21556374
Lowther et al (2011) Endocytosis in the mouse oocyte and its contribution to cAMP signaling during meiotic arrest. Reproduction 141 737 PMID: 21411693
Solé et al (2019) The MAP1B Binding Domain of Nav1.6 Is Required for Stable Expression at the Axon Initial Segment. J Neurosci 39 4238 PMID: 30914445
Pitt et al (2017) Neuroprotective astrocyte-derived Ins/IGF-1 stimulates endocytic processing and extracellular release of neuron-bound Aβ oligomers. Mol Biol Cell 28 2623 PMID: 28963439
Falgairolle and O'Donovan (2015) Pharmacological Investigation of Fluoro-Gold Entry into Spinal Neurons. Eur J Cell Biol 10 e0131430 PMID: 26102354
Petermann et al (2015) Role of Nectin-1 and Herpesvirus Entry Mediator as Cellular Receptors for Herpes Simplex Virus 1 on Primary Murine Dermal Fibroblasts. J Virol 89 9407 PMID: 26136572
Rahn et al (2011) Entry pathways of herpes simplex virus type 1 into human keratinocytes are dynamin- and cholesterol-dependent. PLoS One 6 e25464 PMID: 22022400
Yang et al (2011) Measurement and analysis of traction force dynamics in response to vasoactive agonists. Integr Biol (Camb) 3 663 PMID: 21445393
Proszynski et al (2009) Podosomes are present in a postsynaptic apparatus and participate in its maturation. PLoS One 106 18373 PMID: 19822767
Kolpak et al (2009) Negative guidance factor-induced macropinocytosis in the growth cone plays a critical role in repulsive axon turning. Invest Ophthalmol Vis Sci 29 10488 PMID: 19710302
Li et al (2009) Activation of glycogen synthase kinase-3 β is required for hyperDA and D2 receptor-mediated inhibition of synaptic NMDA receptor function in the rat prefrontal cortex. Mol Biol Cell 29 15551 PMID: 20007479
Khatua et al (2015) Exon 4-encoded sequence is a major determinant of cytotoxicity of apolipoprotein L1. Am J Physiol Cell Physiol 309 C22 PMID: 25924622
Pribiag and Stellwagen (2013) TNF-α Downregulates Inhibitory Neurotransmission through Protein Phosphatase 1-Dependent Trafficking of GABAA Receptors. J Neurosci 33 15879 PMID: 24089494
Marcello et al (2013) Endocytosis of synaptic ADAM10 in neuronal plasticity and Alzheimer's disease. J Clin Invest 123 2523 PMID: 23676497
Bassani et al (2012) The X-linked intellectual disability protein TSPAN7 regulates excitatory synapse development and AMPAR trafficking. Neuron 73 1143 PMID: 22445342
Chandrasekaran et al (2012) HIV-1 Nef impairs heterotrimeric G-protein signaling by targeting Gα(i2) for degradation through ubiquitination. J Biol Chem 287 41481 PMID: 23071112
Hollidge et al (2012) Orthobunyavirus entry into neurons and other mammalian cells occurs via clathrin-mediated endocytosis and requires trafficking into early endosomes. J Virol 86 7988 PMID: 22623766
Lee et al (2012) Actin-dependent rapid recruitment of reluctant synaptic vesicles into a fast-releasing vesicle pool. Proc Natl Acad Sci U S A 109 E765 PMID: 22393020
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We used dynasore inhibitor to investigate the mechanism underlying cellular entry of bacterial membrane vesicles. Human macrophages were treated by 20 uM dynasore for 1 h before adding the fluorescent dye-labeled vesicles for additional 2 h. The fluorescence of vesicles within macrophages was detected by using confocal microscopy. Our observation indicated that pretreatment of cells with dynasore significantly blocked the cellular entry of bacterial membrane vesicles.
100 μM, 45 min