A cell-permeable, reversible, and selective inhibitor of the phosphorylation of Akt and its in vitro kinase activity (complete inhibition <5 M) with minimal effect on PI 3-K, PDK1, or SGK1. Shown to suppress growth of Rh (rhabdomyosarcoma) cell lines (IC50 = 2-5 M), inhibit IGF-I-stimulated nuclear translocation of Akt, and prevent phosphorylation of the downstream targets, mTOR, p70S6 kinase, and S6 ribosomal protein. Unlike Akti1/2, the mode of inhibition is not PH domain-dependent. Also shown to induce neuronal autophagy in an Akt- and mTOR-independent manner and enhances the clearance of misfolded protein. The solid form of this compound is also available.
生化/生理作用
Cell permeable: yes
Primary Target Akt
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
外形
A 20 mM (2 mg/262 µL) solution of Akt Inhibitor X (Cat. No. 124020) in H₂O.
重悬
Following initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
其他说明
Tsvetkov, A.S., et al. 2010. Proc. Natl. Acad. Sci. USA107, 16982. Thimmaiah, K.N., et al. 2005. J. Biol. Chem.280, 31924.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany