Akt Inhibitor XIX, 3CAI

A cell-permeable chloroacetyl-indole compound that inhibits Akt1 and Akt2 kinase activity (IC₅₀<1 µM) by directly targeting Akt PH domain, exhibiting little or much reduced activity against a panel of 84 other kinases, including PI-3 Kinase (60% inhibition at 10 µM). Effectively inhibits Akt-mediated cellular GSK3β Ser⁹ and mTOR Ser²⁴⁴⁸ phosphorylation (4 µM in HCT116 cultures) in a time-dependent manner, resulting in effective apoptosis induction in HCT116 and HT29 cultures (by 55% and 60%, respectively; 4 µM for 4 days). Reported to retard HCT116-derived tumor growth by 50% when administered at an oral dosage of 30 mg/kg in mice (5 times/wk for 3 wks) in vivo.

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Kim, D.J., et al. 2011. Cancer Prev. Res.4, 1842.

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