INTEGRIN #V#3 ANTAGONIST, P1 1PC X 5MG

General description

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.

Legal Information

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

Other Notes

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.

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

Supplied as a trifluoracetate salt.

Reconstitution

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

Warning

Toxicity: Standard Handling (A)