GKI-1是Greatwall(GWL)激酶抑制剂，抑制hGWLFL和hGWL-KinDom的IC50分别为4.9和2.5µM。GKI-1可高效抑制ROCK1，IC50为11µM,仅微弱抑制PKA。
货号:ajcx13470
CAS:2444764-03-6
分子式:C15H12ClN3
分子量：269.73
溶解度:DMSO: 200 mg/mL (741.48 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.