Integrin αvβ3 Antagonist, P11

A cell-permeable, hexapeptide containing a novel integrin-binding motif, SDV (a Type I PDZ-binding motif) that is shown to compete with vitronectin for the RGD-binding site of integrin αvβ3 (IC₅₀ = 1.74 pg/ml), in a chip-based assay. It is rapidly internalized into HUVECs, but not in NIH 3T3 cells, at a culture temperature of 37 °C, a process which is mediated by caveolin and clathrin. At 10 µg/ml, this compound is shown to significantly inhibit the phosphorylation of ERK1/2 and MEK in HUVECs. Furthermore, it suppresses bFGF-induced proliferation of HUVECs, dose-dependently, and displays up-regulation of p53 and induction of apoptosis via activation of caspases-3, -8 and -9 at 50 µg/ml.

Packaged under inert gas

Supplied as a trifluoracetate salt.

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Bang, J., et al. 2011. Mol Cell Proteomics10, M110.
Choi, Y., et al. 2010. Proteomics10, 72.
Lee, Y., et al. 2004. J. Biomol. Screen.9, 687.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)