Name | Thienopyridone |
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Description | 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]. |
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Related Catalog | |
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]. Cell Viability Assay[1] Cell 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 Analysis[1] Cell 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. |
References |
Molecular Formula | C13H10N2OS |
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Molecular Weight | 242.30 |