RGD (Arg-Gly-Asp) is a tripeptide that is the most common peptide motif responsible for cell adhesion to the ECM-extracellular matrix.

GLPG0187 (GLPG-0187) is a novel, potent, broad spectrum and small molecule integrin receptor antagonist (IRA) with potential anticancer activity, inhibiting αvβ1-integrin with an IC50 of 1.3 nM.

Cyclo(-RGDfK) is a potent, selective and cyclo-peptide-based αvβ3 integrin inhibitor with potential antitumor activity.

Tirofiban (also known as L700462 or MK383) is a novel non-peptide antagonist of glycoprotein IIb/IIIa (integrins alphaIIbbetaIII) that is used as an antiplatelet drug.

Cyclo(RGDyK) TFA, the trifluoroacetate (TFA) salt of Cyclo(RGDyK) which is a glycosylated RGD-containing peptide (RGD-peptide), is a potent and selective αVβ3 integrin inhibitor with potential antineoplastic activity.

Lifitegrast (formerly SAR 1118; SAR 1118-023; SAR-1118; trade name Xiidra) is a novel and potent integrin lymphocyte function-associated antigen-1 (LFA-1) antagonist approved in 2016 for the the treatment of Dry Eye Disease.

OSU-T315 (1,5-regioisomer) is a novel, potent and specific small molecule inhibitor of Integrin-linked kinase (ILK) with an IC50 of 0.6 μM, suppressing cancer cell proliferation in vitro and in vivo and inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain).

A-205804 (A205804; A 205804) is a novel selective inhibitor of E-selectin and intercellular adhesion molecule-1 (ICAM-1) expression (IC50 = 20 nM and 25 nM) with potential anticancer activity.