TC-I 15 is a highly potent, selective, allosteric small-molecule inhibitor of integrin α2β1 with IC50 of 12 nM.
TC-I 15 inhibits adhesion of cells expressing wild-type (WT) and demonstrates no effect on RBL cells expressing an activating I-domain mutation (E318A).
TC-I 15 inhibits an activating cytoplasmic domain mutant [Del(GFFKR)] with an IC50 ≈4-fold higher than for wild-type integrin α2β1.
TC-I 15 shows efficacious activity in an animal model of arterial thrombosis.
