Thienopyridone |
カタログ番号GC60364 |
チエノピリドンは、PRL-1、PRL-2、および PRL-3 に対してそれぞれ 173 nM、277 nM、および 128 nM の IC50 を持つ、強力かつ選択的な再生肝ホスファターゼ (PRL) ホスファターゼ阻害剤です。チエノピリドンは、他のホスファターゼにほとんど影響を与えません。チエノピリドンは、p130Cas の切断とアポトーシスを誘導し、抗がん効果があります。
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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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