Catalog No.: PC-20557Not For Human Use, Lab Use Only.
GKI-1 (Greatwall Kinase Inhibitor-1) is a specific small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like, Greatwall/GWL) with IC50 of 10.2 uM.
GKI-1 (Greatwall Kinase Inhibitor-1) is a specific small-molecule inhibitor of MASTL (microtubule-associated serine/threonine kinase-like, Greatwall/GWL) with IC50 of 10.2 uM.
GKI-1 inhibits hGWLFL and hGWL-KinDom with IC50 of 4.9 and 2.5 μM respectively.
GKI-1 displays 2-fold selectivity for binding to hGWLFL over ROCK1, and > 8-fold selectivity over PKA.
GKI-1 reduces ENSA/ARPP19 phosphorylation levels in HeLa cells, resulting in a decrease in mitotic events, mitotic arrest/cell death and cytokinesis failure, which is comparable to siRNA depletion of GWL.
Physicochemical Properties
M.Wt
269.73
Formula
C15H12ClN3
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
N-(4-chlorophenyl)-3-(1H-pyrazol-4-yl)aniline
References
1. Ocasio CA, et al. Oncotarget. 2016 Nov 1;7(44):71182-71197.
2. Kim AY, et al. Front Oncol. 2020 Sep 29;10:571601.
