PI3K/AKT-IN-2 (Compound 12c) is a PI3K and AKT inhibitor. PI3K/AKT-IN-2 blocks the epithelial-mesenchymal transition (EMT) and induces apoptosis. PI3K/AKT-IN-2 inhibits the polymerization of tubulin [1].
In Vitro, PI3K/AKT-IN-2 (Compound 12c) shows antiproliferative activity with IC50 values of 14.84 ± 1.53, 4.79 ± 0.71, 14.34 ± 0.57, 0.89 ± 0.023, >100 and 98.75 ± 1.59 µM against H460, MCF-7, A549, HGC-27, 293 T and GES-1 cells, respectively[1]. PI3K/AKT-IN-2 suppresses the expressions/activities of matrix metalloprotease (MMP)− 2, vimentin and up-regulation E-cadherin[1]. PI3K/AKT-IN-2 induces significant up-regulation of CDK1 proteins expression with a down-regulation of cyclin B1 and Cdc25C[1].
References:
[1]. Sun W, et al. Design, semi-synthesis and bioactivity evaluation of novel podophyllotoxin derivatives as potent anti-tumor agents. Bioorg Chem. 2022 May 26;126:105906.
In Vitro, PI3K/AKT-IN-2 (Compound 12c) shows antiproliferative activity with IC50 values of 14.84 ± 1.53, 4.79 ± 0.71, 14.34 ± 0.57, 0.89 ± 0.023, >100 and 98.75 ± 1.59 µM against H460, MCF-7, A549, HGC-27, 293 T and GES-1 cells, respectively[1]. PI3K/AKT-IN-2 suppresses the expressions/activities of matrix metalloprotease (MMP)− 2, vimentin and up-regulation E-cadherin[1]. PI3K/AKT-IN-2 induces significant up-regulation of CDK1 proteins expression with a down-regulation of cyclin B1 and Cdc25C[1].
References:
[1]. Sun W, et al. Design, semi-synthesis and bioactivity evaluation of novel podophyllotoxin derivatives as potent anti-tumor agents. Bioorg Chem. 2022 May 26;126:105906.