Thienopyridone is a potent and selective inhibitor of phosphatase of regenerating liver (PRL) phosphatase [IC50 values of 173 nM for PRL-1, 277 nM for PRL-2, and 128 nM for PRL-3], and induces p130Cas cleavage and apoptosis with anticancer effects.

PRL2:277 nM , PRL3:128 nM , PRL1:173 nM

in soft agar, Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth (EC50 of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively). Thienopyridone (1-75 μM; 24 hours; HeLa cells) treatment shows a dose-dependent down-regulation of total p130Cas in HeLa cells. Thienopyridone induces p130Cas and FAK cleavage leads to caspase-mediated cell apoptosis. the cleavage of PARP and caspase-8 induced by Thienopyridone. Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation.