IA-0130 a specific glycoprotein 130 (gp130, IL-6Rβ) inhibitor with SPR KD of 2.8 uM, interfers with the interaction between IL-6 and gp130, inhibits IL-6/gp130/STAT3 pathway activity.
IA-0130 directly binds to gp130 in a dose-dependent manner but not to IL-6 and IL-6Rα.
IA-0130 significantly inhibits IL-6-induced SEAP secretion in a concentration-dependent manner with IC50 of 4.77 uM in HEK-blue™ IL-6 cells.
IA-0130 down-regulated IL-6 expression and prevented the phosphorylation of signaling molecules in colonic tissues.
IA-0130 suppressed colitis progression by inhibiting the gp130 signaling pathway and expression of pro-inflammatory cytokines, and maintaining TJ integrity.
IA-0130 inhibited gp130/STAT3 phosphorylation in a concentration-dependent manner in ovarian cancer cell line and also in ovarian cancer-resistant cell line.
IA-0130 inhibits tumour growth, migration and metastasis by inhibiting IL-6/gp130/STAT3 signalling in ovarian cancer by binding gp130.