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GSK690693 is a pan-Akt inhibitor targeting Akt1, 2, 3 with IC50 values of 2, 13 and 9 nM, respectively [1, 2]. In addition, it also inhibits AMPK (IC50=50 nM), DAPK3 (IC50=81 nM), PAK4, 5, and 6 (IC50=10, 52, 6 nM), as well as the members of AGC kinase family including PKA (IC50=24 nM), PrkX (IC50=5 nM), and PKC isozymes (IC50=2-21 nM) [1]. GSK690693 reversibly occupies the ATP binding pocket of the kinase domain and competes with ATP as shown by crystal structure [2]. It blocks the phosphorylation of downstream targets of ATK in a dose-dependent manner [1].

GSK690693 has shown potential anti-tumor activity both in vitro and in vivo.

Akt plays an important role in regulation of cell cycle progression and tumor cell survival. GSK690693 reduced proliferation and led to apoptosis in tumor cells with potency correlated to the inhibited activity of Akt kinase [1, 3]. In xenografts models, it inhibited the growth of SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast tumors [1]. It delayed the tumor progression in transgenic mice expressing a constitutively activated form of Akt [4]. GSK690693 has been tested in phase I clinical trials [5].

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