GSK2256098 (GTPL-7939) is a potent, selective, reversible and ATP-competitive inhibitor of FAK kinase with Ki of 0.4 nM.
GSK2256098 (GTPL-7939) dispalys high selectivity over a panel of 261 kinases, including the nearest FAK family member, Pyk2 (>1,000-fold).
GSK2256098 (GTPL-7939) inhibits FAK activity through targeting the phosphorylation site of FAK Y397.
GSK2256098 (GTPL-7939) decreases levels of phosphorylated Akt and ERK, cell viability, anchorage-independent growth, and motility in L3.6P1 cells.
GSK2256098 (GTPL-7939) causes lower microvessel density, less cellular proliferation, and higher apoptosis rates in the Ishikawa model.
