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Submit ReviewCilengitide is a potent and selective inhibitor of integrins αvβ3 and αvβ5 (IC50 values are 4.1 and 70 nM, respectively). Exhibits ~10-fold selectivity over gpIIb/IIIa. Increases endothelial monolayer permeability. Also exhibits antiangiogenic activity.
分子量 | 588.66 |
公式 | C27H40N8O7 |
序列 |
RGDFV (Modifications: Phe-4 = D-Phe, Val-5 = Me-Val, Cyclized) |
储存 | Store at -20°C |
纯度 | ≥95% (HPLC) |
CAS Number | 188968-51-6 |
PubChem ID | 176873 |
InChI Key | AMLYAMJWYAIXIA-VWNVYAMZSA-N |
Smiles | CC(C)[C@H]1C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@@H](C(=O)N1C)CC2=CC=CC=C2)CC(=O)O)CCCN=C(N)N |
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.
溶解性 | Soluble to 10 mg/ml in water |
参考文献是支持产品生物活性的出版物。
Alghisi et al (2009) The integrin antagonist cilengitide activates αvβ3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells. PLoS One 4 e4449 PMID: 19212436
Monnier et al (2008) CYR61 and αvβ5 integrin cooperate to promote invasion and metastasis of tumors growing in preirradiated stroma. Cancer Res. 68 7323 PMID: 18794119
If you know of a relevant reference for Cilengitide, please let us know.
关键词: Cilengitide, Cilengitide supplier, Potent, selective, inhibitors, inhibits, integrin, αvβ3, αvβ5, alphavbeta3, alphavbeta5, EMD121974, Integrins, Cell, Adhesion, Molecules, 5870, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Cilengitide 的部分引用包括:
Filla et al (2019) Activation of αvβ3 Integrin Alters Fibronectin Fibril Formation in Human Trabecular Meshwork Cells in a ROCK-Independent Manner. Invest Ophthalmol Vis Sci 60 3897 PMID: 31529121
Lee et al (2019) Extracorporeal shock waves protect cardiomyocytes from DOX-induced cardiomyopathy by upregulating survivin via the integrin-ILK-Akt-Sp1/p53 axis. Sci Rep 9 12149 PMID: 31434946
Elazer R et al (2019) Subendothelial matrix components influence endothelial cell apoptosis in vitro. Am J Physiol Cell Physiol 316 C210-C222 PMID: 30566394
Albarrán-Juárez et al (2018) Piezo1 and Gq/G11 promote endothelial inflammation depending on flow pattern and integrin activation. J Exp Med 215 2655 PMID: 30194266
Adriano et al (2022) G protein-coupled receptor kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by chemokine receptor CXCR4. J Biol Chem 298 102351 PMID: 35940305
Jerzy W et al (2022) Integrins Bidirectionally Regulate the Efficacy of Inhibitory Synaptic Transmission and Control GABAergic Plasticity. J Neurosci 42 5830-5842 PMID: 35701161
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