| Description | GKI-1 is a Greatwall (GWL) kinase inhibitor that inhibits hGWLFL with an IC50 of 4.9. GKI-1 also inhibited hGWL-KinDom, and its IC50 was 2.5 µM. The inhibitory effect of GKI-1 on ROCK1 was better than that of hGWLFL and hGWL-KinDom, and its IC50 was 11 µM, which only weakly inhibited PKA. |
| In vitro | Treatment of HeLa cells with GKI-1 (25 and 50µM, 0-8.5 h) reduced ENSA/ARPP19 phosphorylation levels, resulting in reduced mitotic events, mitotic arrest/cell death, and cell division failure. GKI-1 inhibited full-length human GWL and showed cellular effects[1] |
| Target activity | GWL-KinDom (human):4.9 µM , GWLFL (human):4.9 µM , GWLFL (human):4.9 µM, GWL-KinDom (human):2.5 µM, ROCK1:11 µM |
| molecular weight | 269.73 |
| Molecular formula | C15H12ClN3 |
| CAS | 2444764-03-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 180.0 mg/mL (667.3 mM), Sonication is recommended. |
| References | 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. |