Cilengitide

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Cat.No. 5870 - Cilengitide | cyclo(Arg-Gly-Asp-D-Phe-(NMe)-Val) | CAS No. 188968-51-6
Description: Potent and selective inhibitor of integrins αvβ3 and αvβ5
Alternative Names: EMD121974
Datasheet
Citations (3)
Reviews
Literature (3)

Biological Activity

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

M. Wt 588.66
Formula C27H40N8O7
Sequence RGDFV

(Modifications: Phe-4 = D-Phe, Val-5 = Me-Val, Cyclizedl)

Storage Store at -20°C
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

Solubility Soluble to 10 mg/ml in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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View all Integrin Inhibitors

Keywords: Cilengitide, Cilengitide supplier, Potent, selective, inhibitors, inhibits, integrin, αvβ3, αvβ5, alphavbeta3, alphavbeta5, EMD121974, Integrins, Cell, Adhesion, Molecules, 5870, Tocris Bioscience

3 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


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The Tocris chemistry team has considerable chemistry knowledge and skill which it has recently been applying to the generation of new chemical probes from known tools and compounds to help answer biological questions. This poster presents some of the work carried out by Tocris scientists and focuses on two areas: the generation of libraries of chemical building blocks to support Degrader (PROTAC) research and the development of a fluorescent probe to study integrin biology. Presented at Chemical Tools for Complex Biological Systems II, 2019, Janelia Research Campus, USA.