GKI-1 |
| カタログ番号GC34381 |
GKI-1 は、hGWLFL および hGWL-KinDom に対してそれぞれ 4.9 μM および 2.5 μM の IC50 を持つ Greatwall (GWL) キナーゼ阻害剤です。 GKI-1 は ROCK1 を 11 μM の IC50 で強力に阻害しますが、PKA にはわずかにしか影響しませんでした。
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Cas No.: 2444764-03-6
Sample solution is provided at 25 µL, 10mM.
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GKI-1 is a Greatwall (GWL) kinase inhibitor with IC50s of 4.9 and 2.5 µM against hGWLFL and hGWL-KinDom, respectively. GKI-1 robustly inhibits ROCK1 with an IC50 of 11 µM, but only weakly affected PKA[1].
GKI-1 inhibits full-length human GWL, and shows cellular efficacy[1]. Treatment of HeLa cells (25 and 50 µM) with GKI-1 reduces ENSA/ARPP19 phosphorylation levels, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure[1].
[1]. Ocasio CA, et al. A first generation inhibitor of human Greatwall kinase, enabled by structural and functional characterisation of a minimal kinase domain construct. Oncotarget. 2016 Nov 1;7(44):71182-71197.
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