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 avb3 (IC50=1.74pg/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 10u/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 50ug/ml.
Formula:C₃₀H₅₁N₁₂O₉₃· 3TFA
Molecular Weight:1062.9
Solubility:H2O (100mg/ml)
Purity:≥95% (HPLC)
Form:Supplied as a white solid.
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile ddH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
