PI3K/AKT-IN-2

• CAT Number: I043653
• CAS Number: 2684412-41-5
• Molecular Formula: C32H27BrO10
• Molecular Weight: 651.45
• Purity: ≥95%
• Synonyms: [(5R,5aR,8aR,9R)-8-oxo-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[5,6-f][1,3]benzodioxol-5-yl] (E)-4-(4-bromophenyl)-4-oxobut-2-enoate
• InChI: InChI=1S/C32H27BrO10/c1-37-25-10-17(11-26(38-2)31(25)39-3)28-19-12-23-24(42-15-41-23)13-20(19)30(21-14-40-32(36)29(21)28)43-27(35)9-8-22(34)16-4-6-18(33)7-5-16/h4-13,21,28-30H,14-15H2,1-3H3/b9-8+/t21-,28+,29-,30-/m0/s1
• InChIKey: IKTFRKYEGUKRPW-NHMJTRFWSA-N
• SMILES: COC1=CC(=CC(=C1OC)OC)C2C3C(COC3=O)C(C4=CC5=C(C=C24)OCO5)OC(=O)C=CC(=O)C6=CC=C(C=C6)Br

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].
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].

Reference

[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.
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