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Submit ReviewCilengitide
Description: Potent and selective inhibitor of integrins αvβ3 and αvβ5
Alternative Names: EMD121974
Purity: ≥95% (HPLC)
Biological Activity for Cilengitide
Cilengitide 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.
Technical Data for Cilengitide
| M. Wt | 588.66 |
| Formula | C27H40N8O7 |
| Sequence |
RGDFV (Modifications: Phe-4 = D-Phe, Val-5 = Me-Val, Cyclized) |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Cilengitide
| Solubility | Soluble to 10 mg/ml in water |
Product Datasheets for Cilengitide
References for Cilengitide
References are publications that support the biological activity of the product.
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.
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Keywords: Cilengitide, Cilengitide supplier, Potent, selective, inhibitors, inhibits, integrin, αvβ3, αvβ5, alphavbeta3, alphavbeta5, EMD121974, Integrins, Cell, Adhesion, Molecules, 5870, Tocris Bioscience
6 Citations for Cilengitide
Citations are publications that use Tocris products. Selected citations for Cilengitide include:
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
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
Elazer R et al (2019) Subendothelial matrix components influence endothelial cell apoptosis in vitro. Am J Physiol Cell Physiol 316 C210-C222 PMID: 30566394
Do you know of a great paper that uses Cilengitide from Tocris? Please let us know.
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