GSK2256098 [2-[5-Chloro-2-(2-isopropyl-5-methyl-2H-pyrazol-3-yiamino)-pyridin-4-ylamino]-N-methoxy-benzamide] as a potent,
selective, reversible, and ATP competitive inhibitor of FAK (Focal adhesion
kinase) activity (apparent Ki =
0.4 nM). The cocrystal structure reveals compound bound in the ATP binding
pocket of FAK [1].
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| GSK2256098: 2D and 3D Structure |
The potent enzymatic activity translates to cellular activity when IC50 values for reducing cellular phospho-FAK levels (pFAK-(Tyr 397)) were determined by ELISA. GSK2256098 inhibited cellular pFAK with IC50 values from 2-15 nM and level of pFAK remained low over time in the continues presence of the compound [1].
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| 1H NMR (Estimated) for GSK2256098 |
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