Thienopyridone |
Katalog-Nr.GC60364 |
Thienopyridon ist ein potenter und selektiver Phosphatase-Inhibitor der Phosphatase der regenerierenden Leber (PRL) mit IC50-Werten von 173 nM, 277 nM und 128 nM fÜr PRL-1, PRL-2 bzw. PRL-3. Thienopyridon zeigt minimale Wirkungen auf andere Phosphatasen. Thienopyridon induziert p130Cas-Spaltung und Apoptose und hat Antikrebswirkungen.
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Cas No.: 1018454-97-1
Sample solution is provided at 25 µL, 10mM.
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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