RGDS peptide (Arg-Gly-Asp-Ser) is a integrin binding sequence that inhibits integrin receptor function, a tetrapeptide analogue of the cell attachment site of fibronectin.

Lifitegrast sodium (SAR-1118-023 sodium) is a small molecule integrin antagonist that inhibits T cell-mediated inflammation by blocking the binding of two important cell surface proteins (lymphocyte function-associated antigen 1 and intercellular adhesion molecule 1), which reduces inflammation of the ocular surface, and may be used in the study of dry eye.

α2β1 integrin-IN-15 highly potent, selective, allosteric small-molecule inhibitor of integrin α2β1 with IC50 of 12 nM.