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详细内容
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AKT-IN-3 (compound E22) is a potent, orally active low hERG blocking Akt inhibitor, with 1.4 nM, 1.2 nM and 1.7 nM for Akt1, Akt2 and Akt3, respectively. AKT-IN-3 (compound E22) also exhibits good inhibitory activity against other AGC family kinases, such as PKA, PKC, ROCK1, RSK1, P70S6K, and SGK. AKT-IN-3 (compound E22) induces apoptosis and inhibits metastasis of cancer cells[1]. Akt1|1.4 nM (IC50)|Akt2|1.2 nM (IC50)|Akt3|1.7 nM (IC50)|PKA|0.3 nM (IC50)|P70S6K|8.9 (IC50)
[1]. Dong X, et al. Discovery of 3,4,6-Trisubstituted Piperidine Derivatives as Orally Active, Low hERG Blocking Akt Inhibitors via Conformational Restriction and Structure-Based Design. J Med Chem. 2019 Aug 8;62(15):7264-7288.
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