Akt functions as a key component in multiple signaling pathways to promote cell survival by mediating resistance to apoptosis. Akt inhibitor X is a cell permeable phenoxazine derivative that suppresses insulin-like growth factor 1 (IGF-1)-stimulated phosphorylation of Akt with an IC50 value of 1-2 μM. This compound has been shown to block IGF-1-stimulated nuclear translocation of Akt in Rh1 cells and to inhibit the growth of Rh1, Rh18, and Rh30 cells with IC50 values of 2-5 μM. Inhibition of Akt phosphorylation by 5 μM of this compound strongly correlates to the inhibition of the downstream targets, mTOR, p70S6 kinase, and S6 ribosomal protein and to an increase in apoptosis.
Akt Inhibitor X is used as a cell-permeable, reversible, and selective inhibitor of the phosphorylation of Akt and its in vitro kinase activity.
[1]. janjetovic k, vucicevic l, misirkic m, et al. metformin reduces cisplatin-mediated apoptotic death of cancer cells through ampk-independent activation of akt. european journal of pharmacology, 2011, 651(1): 41-50.
[2]. de abreu la, calixto c, waltero cf, et al. the conserved role of the akt/gsk3 axis in cell survival and glycogen metabolism in rhipicephalus (boophilus) microplus embryo tick cell line bme26. biochimica et biophysica acta (bba)-general subjects, 2013, 1830(3): 2574-2582.
[3]. brunet a, bonni a, zigmond mj, et al. akt promotes cell survival by phosphorylating and inhibiting a forkhead transcription factor. cell, 1999, 96(6): 857-868.
[4]. pulinilkunnil t, he h, kong d, et al. adrenergic regulation of amp-activated protein kinase in brown adipose tissue in vivo. journal of biological chemistry, 2011, 286(11): 8798-8809.
