THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2[1].
In cell adhesion assays in which Jurkat cells bound to CS1-conjugated BSA, THI0019 shows a dose-dependent enhancement in cell binding with an EC50 of 1.7 μM. When VCAM-1 is used as the ligand, THI0019 induces an even more pronounced 100-fold increase in Jurkat cell binding, with an EC50 of 1.2 μM. THI0019 induces a dose-dependent increase in EPC binding to VCAM-1 (EC50 of 3.7 μM). THI0019 facilitates the rolling and spreading of cells on VCAM-1 and the migration of cells toward SDF-1α[1].
[1]. Peter Vanderslice, et al. Small molecule agonist of very late antigen-4 (VLA-4) integrin induces progenitor cell adhesion. J Biol Chem. 2013 Jul 5;288(27):19414-28.