Norleual

Norleual, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC₅₀ of 3 pM. Norleual is an AT4 receptor antagonist and exhibits potent antiangiogenic activities^[1]. In Vitro: Norleual at 20 and 50 pM significantly reduces HGF-dependent c-Met and Gab1 phosphorylation. 20 pM Norleual dramatically reduces HGF-initiated association between Gab1 and c-Met in HEK293 cells. Norleual markedly attenuates HGF-dependent c-Met activation and downstream signaling^[1]. Norleual (1 pM-1 μM; 4 days) is able to inhibit HGF-dependent signaling, proliferation, migration, and invasion in multiple cell types at concentrations in the picomolar range in MDCK cells^[1]. In Vivo: Norleual (50 μg/kg; intraperitoneal injection; daily; for 2 weeks; C57BL/6 mice) suppresses pulmonary colonization by B16-F10 murine melanoma cells^[1].