Dynasore
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
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. 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
- 2. 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.
- 3. 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
- 4. 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
- 5. 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
相关生物数据
相关生物数据
相关生物数据
