Thienopyridone |
| Catalog No.GC60364 |
La thiénopyridone est une phosphatase puissante et sélective de la phosphatase hépatique régénérante (PRL) avec des IC50 de 173 nM, 277 nM et 128 nM pour PRL-1, PRL-2 et PRL-3, respectivement. La thiénopyridone montre des effets minimes sur les autres phosphatases. La thiénopyridone induit le clivage et l'apoptose de p130Cas et a des effets anticancéreux.
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Cas No.: 1018454-97-1
Sample solution is provided at 25 µL, 10mM.
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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].
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
[1]. Daouti S, et al. A selective phosphatase of regenerating liver phosphatase inhibitor suppresses tumor cell anchorage-independent growth by a novel mechanism involving p130Cas cleavage. Cancer Res. 2008 Feb 15;68(4):1162-9.
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