| Bioactivity | 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]. |
| Target | IC50: 4.9 µM (hGWLFL), 4.9 µM (hGWL-KinDom) |
| Invitro | GKI-1 inhibits full-length human GWL, and shows cellular efficacy[1]. 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[1]. |
| Name | GKI-1 |
| CAS | 2444764-03-6 |
| Formula | C15H12ClN3 |
| Molar Mass | 269.73 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [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. |