GB2095

GB2095 is an orally active and selective galectin-3 inhibitor. GB2095 shows superior selectivity for both human (K_D = 0.036 μM) and mouse galectin-3 (K_D = 0.35 μM) over other galectins (such as h-Gal-1/4N/4C/8N/8C/9N/9C and m-galectin-1). GB2095 inhibits tumor growth in syngeneic mouse models of breast and melanoma cancers. GB2095 can be used for breast and melanoma cancer research^[1]. IC50 & Target:K_d: 36 nM (human galectin-3); 0.35 μM (mouse galectin-3) In Vitro:GB2095 displays a 14-fold selectivity for human galectin-3 over the other tested human galectins (Gal-1, -4N, -4C, -8N, -8C, -9N, -9C) on average, and shows a more pronounced (100-fold) selectivity for mouse galectin-3 over mouse galectin-1^[1].
GB2095 shows high permeability and no efflux over a CACO-2 cell monolayer, alongside good hepatic stability in both humans and mice, and exhibits moderate plasma protein binding in both human and mouse plasma^[1]. In Vivo:GB2095 (30 mg/kg, p.o., b.i.d from day 1 to day 14 or 25) inhibits tumor growth in breast (4T1) and melanoma (B16-F10) syngeneic mice models^[1].