CDE-096 is a potent inhibitor of PAI-1. CDE-096 prevents PAI-1 from inactivating tPA and uPA with similar potency (IC50=30 and 25 nM, respectively) and is active against glycosylated PAI-1, as well as PAI-1 derived from several species (IC50=19, 22 and 18 nM for murine, rat, and Porcine PAI-1, respectively)[1].
CDE-096 is active against both free PAI-1 and vitronectin-bound PAI-1. CDE-096 binds to PAI-1 with nanomolar affinity and induces conformational changes that prevent binding to both proteases and vitronectin[1].
[1]. Li SH, et al. Mechanistic characterization and crystal structure of a small molecule inactivator bound to plasminogen activator inhibitor-1. Proc Natl Acad Sci U S A. 2013;110(51):E4941-E4949.