Dynasore
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mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
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Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
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Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
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Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
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SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Dynasore是一种非竞争性的GTP酶抑制剂,IC50值为15 μM[1][2]。
GTP酶(单GTP酶)是水解酶,在GTP的结合和水解中起重要作用。GTP酶参与许多过程,如信号转导、蛋白生物合成、蛋白的细胞膜易位以及细胞内小泡的运输。据报道,dynasore可抑制dynamin1、dynamin2和Drp1的GTP酶活性[3] [4]。
Dynasore是一种有效的GTP酶抑制剂,作用于dynamin1、dynamin2或Drp1上的位点。在HL-1细胞中,dynasore通过抑制动力素的活性,阻断内吞过程[1]。用遗传编码pH敏感的荧光探针synaptopHluorin来研究动力素在表达spH的突触中的作用,结果表明,dynasore通过减少动力素的GTP酶活性,导致正常刺激触发的荧光强度的增加,从而阻断突触内吞作用[4]。Dynasore作为动力素GTP酶活性的抑制剂,可阻断细胞和神经元中动力素依赖的内吞作用[3]。
参考文献:
[1]. Zheng, J., et al., Chymase mediates injury and mitochondrial damage in cardiomyocytes during acute ischemia/reperfusion in the dog. PLoS One, 2014. 9(4): p. e94732.
[2]. McCluskey, A., et al., Building a better dynasore: the dyngo compounds potently inhibit dynamin and endocytosis. Traffic, 2013. 14(12): p. 1272-89.
[3]. Kirchhausen, T., E. Macia, and H.E. Pelish, Use of dynasore, the small molecule inhibitor of dynamin, in the regulation of endocytosis. Methods Enzymol, 2008. 438: p. 77-93.
[4]. Newton, A.J., T. Kirchhausen, and V.N. Murthy, Inhibition of dynamin completely blocks compensatory synaptic vesicle endocytosis. Proc Natl Acad Sci U S A, 2006. 103(47): p. 17955-60.
- 1. Xiaohai Song, Hao Cai, et al. "Enzyme‐Responsive Branched Glycopolymer‐Based Nanoassembly for Co‐Delivery of Paclitaxel and Akt Inhibitor toward Synergistic Therapy of Gastric Cancer." Adv Sci (Weinh). 2023 Nov 12:e2306230. PMID: 37953442
- 2. Wei P, Ning M, et al. "Spiroplasma eriocheiris entered Drosophila Schneider 2 cells and relied on clathrin-mediated endocytosis and macropinocytosis." Infect Immun. 2019 Aug 26. pii: IAI.00233-19. PMID:31451616
- 3. Ying Wen, Shouwen Chen, et al."Dysregulated haemolysin promotes bacterial outer membrane vesicles‐induced pyroptotic‐like cell death in zebrafish."Cellular Microbiology. 31 January 2019.
- 4. Wang H, Liu W, et al. "Inhibitor analysis revealed that clathrin-mediated endocytosis is involed in cellular entry of type III grass carp reovirus." Virol J. 2018 May 24;15(1):92. PMID:29793525
- 5. Mai J, Li X, et al. "A DNA Thioaptamer with Homing Specificity to Lymphoma Bone Marrow Involvement." Mol Pharm. 2018 May 7;15(5):1814-1825. PMID:29537266
- 6. Schappe MS, Szteyn K, et al."Chanzyme TRPM7 Mediates the Ca(2+) Influx Essential for Lipopolysaccharide-Induced Toll-Like Receptor 4 Endocytosis and Macrophage Activation." Immunity. 2018 Jan 16;48(1):59-74.e5. PMID:29343440
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 322.31 |
Cas No. | 304448-55-3 |
Formula | C18H14N2O4 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥16.12 mg/mL in DMSO |
Chemical Name | (E)-N'-(3,4-dihydroxybenzylidene)-3-hydroxy-2-naphthohydrazide |
SDF | Download SDF |
Canonical SMILES | OC1=C(C(N/N=C/C(C=C2)=CC(O)=C2O)=O)C=C(C=CC=C3)C3=C1 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
Hela细胞 |
制备方法 |
在DMSO中的溶解度大于16.1 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。 |
反应条件 |
0、1、10、20、40、60和80 μM;30分钟 |
实验结果 |
使用80 μM Dynasore预处理Hela细胞30分钟,转铁蛋白摄取、运输以及胞内积累均被显著抑制。此外,Dynasore呈剂量依赖性地抑制转铁蛋白摄取。实验表明,Dynasore对转铁蛋白摄取的抑制作用是可逆的。 |
References: [1]. Macia E, Ehrlich M, Massol R, Boucrot E, Brunner C, Kirchhausen T. Dynasore, a cell-permeable inhibitor of dynamin. Dev Cell. 2006 Jun;10(6):839-50. |
描述 | Dynasore是一种细胞通透性的和非竞争性的动力素GTP酶抑制剂,IC50值为15 μM。 | |||||
靶点 | dynamin GTPase | |||||
IC50 | 15 ?M |
质量控制和MSDS
- 批次:
化学结构
![Dynasore](http://www.apexbt.com//media/diy/images/struct/A1605.png)
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