Biological ActivityCilengitide 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.
(Modifications: Phe-4 = D-Phe, Val-5 = Me-Val, Cyclized)
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.
The integrin antagonist cilengitide activates αvβ3, disrupts VE-cadherin localization at cell junctions and enhances permeability in endothelial cells.
Alghisi et al.
PLoS One, 2009;4:e4449
CYR61 and αvβ5 integrin cooperate to promote invasion and metastasis of tumors growing in preirradiated stroma.
Monnier et al.
Cancer Res., 2008;68:7323
Citations for Cilengitide
The citations listed below are publications that use Tocris products. Selected citations for Cilengitide include:
6 Citations: Showing 1 - 6
Integrins Bidirectionally Regulate the Efficacy of Inhibitory Synaptic Transmission and Control GABAergic Plasticity.
Authors: Jerzy W Et al.
J Neurosci 2022;42:5830-5842
G protein-coupled receptor kinase phosphorylation of distal C-tail sites specifies βarrestin1-mediated signaling by chemokine receptor CXCR4.
Authors: Adriano Et al.
J Biol Chem 2022;298:102351
Extracorporeal shock waves protect cardiomyocytes from DOX-induced cardiomyopathy by upregulating survivin via the integrin-ILK-Akt-Sp1/p53 axis.
Authors: Lee Et al.
Sci Rep 2019;9:12149
Activation of αvβ3 Integrin Alters Fibronectin Fibril Formation in Human Trabecular Meshwork Cells in a ROCK-Independent Manner.
Authors: Filla Et al.
Invest Ophthalmol Vis Sci 2019;60:3897
Subendothelial matrix components influence endothelial cell apoptosis in vitro.
Authors: Elazer R Et al.
Am J Physiol Cell Physiol 2019;316:C210-C222
Piezo1 and Gq/G11 promote endothelial inflammation depending on flow pattern and integrin activation.
Authors: Albarrán-Juárez Et al.
J Exp Med 2018;215:2655
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