UniPR129 is a potent, selective Eph/ephrin antagonist, competitively disrupts Eph2A-ephrin-A1 binding (IC50=945 nM, Ki = 345 nM).
UniPR129 blocks the interaction of ephrin-A1 and ephrin-B1 with all Eph receptors (IC50 = 840 nM - 1.54 µM for EphA and 2.6 - 3.74 µM for EphB).
UniPR129 inhibits EphA2 phosphorylation in PC3 prostate cancer cells (IC50 = 5 µM), does not affect tyrosine kinase activity of EGF and VEGF receptors.
UniPR129 inhibits angiogenesis in HUVEC (IC50 = 5.2 µM) and reduces ephrin-induced activation of EPhA2 and EphB4 (IC50 = 26.3 and 18.4 µM, respectively).
