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Beschreibung

A cell-permeable, synthetic maleimido-conjugated VIVIT motif peptide (HPVIVIT) that acts as a potent bipartite inhibitor of Nuclear factor of activated T-cells (NFAT) (IC50 = 62 nM). Blocks NFAT-calcineurin interaction by targeting two separate calcineurin docking motifs. Completely blocks NFAT dephosphorylation at 1 mM. Determined to be more potent that Cyclosporine A (Cat. No. 239835) and VIVIT peptide (MAGPHPVIVITGPHEE) in blocking NFAT activity. Also shown to blocks NFAT-mediated T-cell activation and vascular smooth muscle cell proliferation, thereby reducing neoimtima (new thickening of arterial wall) formation in mouse models of restenosis (repeat blocking of blood vessels). The biological half life of MCV1 has been estimated to be about 36 hours in COS-1 cells.