Introduction of 1018454-97-1 :
Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects[1]. IC50 & Target: IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)[1] In Vitro: Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC50 values of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively[1].
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. Thienopyridone induces the cleavage of PARP and caspase-8[1].
Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation[1].
