CCT128930 hydrochloride

CCT128930 is an ATP-competitive inhibitor of Akt2 (IC₅₀ = 6 nM).¹ It is selective for Akt over a panel of 47 other kinases, including the related protein kinase A and p70S6K.¹ CCT128930 blocks the phosphorylation of Akt targets, inhibits proliferation of multiple tumor cell lines in vitro, and prevents the growth of human tumor xenografts in mice.¹ CCT128930 has been used to elucidate the role of Akt2 in regulating the function of interacting proteins, modulating DNA damage and autophagy in HepG2 hepatoma cells, and cell survival and vasculogenesis in endothelial colony forming cells.^2,3,4

1.Yap, T.A., Walton, M.I., Hunter, L.J.K., et al.Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930Mol. Cancer Ther.10(2)360-371(2011) 2.Bottermann, K., Reinartz, M., Barsoum, M., et al.Systematic analysis reveals elongation factor 2 and α-enolase as novel interaction partners of AKT2PLoS One8(6)1-12(2013) 3.Wang, F.Z., Chang, Z.Y., Fei, H.R., et al.CCT128930 induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibitionBiochimie.103118-125(2014) 4.Kim, H., Prasain, N., Vemula, S., et al.Human platelet lysate improves human cord blood derived ECFC survival and vasculogenesis in three dimensional (3D) collagen matricesMicrovasc. Res.10172-81(2015)