MilliporeSigma™ Calbiochem™ Akt Inhibitor XVI, AT7867

Description

• A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC 50 = 32, 17, and 47nM against Akt1, Akt2, and Akt3, respectively), PKA (IC 50 = 20nM), and p70S6K (IC 50 = 85nM) in an ATP-competitive manner (K i = 18nM using AKT2), with much reduced potency toward RSK1 (IC 50 >100nM) and a panel of 13 other cellular kinases (IC 50 >1μM)
• Shown to reduce cellular phosphorylation of GSK-3β (IC 50 range from 2.08 to 4.45μM), S6R, FKHRL1, and inhibit the proliferation of cancer cells exhibiting constitutive Akt pathway activation both in vitro (IC 50 range from 0.94 to 11.86μM) and in mice in vivo (20mg/kg via i.p
• or 90mg/kg via p.o.).