Thienopyridone

Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC 50 s 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 In Vitro Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC 50 values 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. Thienopyridone induces the cleavage of PARP and caspase-8. Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: RKO and HT-29 cells Concentration: 0.5 μM, 1.67 μM, 5 μM, 8.33 μM Incubation Time: 14 days Result: Exhibited a dose-dependent inhibition in cancer cell anchorage-independent growth as measured by either colony number or colony size. Western Blot AnalysisCell Line: HeLa cells Concentration: 1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM Incubation Time: 24 hours Result: A dose-dependent down-regulation of total p130Cas was observed. Form:Solid IC50& Target:IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)

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