AKT-IN-3 (compound E22) 是一种有效、口服的低 hERG 阻断 Akt 抑制剂，对 Akt1、Akt2 和 Akt3 作用的 IC50 值分别为 1.4 nM、1.2 nM 和 1.7 nM。AKT-IN-3 (compound E22) 对其他 AGC 家族激酶也有较好的抑制活性，如 PKA、PKC、ROCK1、RSK1、P70S6K、SGK。AKT-IN-3 (compound E22) 能诱导癌细胞凋亡，抑制癌细胞的转移。
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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