Highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice.

Columbianetin may be helpful in regulating mast cell-mediated allergic inflammatory responses.The absorption of columbianetin acetate is a passive diffusion process without pH-dependent.

5,6-dibromo-1H-indole-3-carboxylic acid is a marine derived natural products found in Smenospongia sp.