Molecular Formula | C15H12ClN3 |
Molar Mass | 269.73 |
Density | 1.320±0.06 g/cm3(Predicted) |
Boling Point | 504.5±45.0 °C(Predicted) |
pKa | 13.93±0.50(Predicted) |
Storage Condition | 2-8°C,惰性气体保存 |
In vitro study | GKI-1 inhibits full-length human GWL, and shows cellular efficacy. Treatment of HeLa cells (25 and 50 µM, 0-8.5 hours) with GKI-1 reduces ENSA/ARPP19 phosphorylation levels, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure. |
biological activity | GKI-1 is a great wall (GWL) kinase inhibitor, the IC50 for the inhibition of hGWLFL and hGWL-KinDom were 4.9 and 2.5 μm, respectively. GKI-1 can effectively inhibit ROCK1,IC50 is 11 M, only a weak inhibition of PKA. |
Target | IC50: 4.9 µm (hGWL FL ), 4.9 µm (hGWL-KinDom) |