PI3K-IN-33

PI3K-IN-33 (Compound 6e) is a highly selective PI3K inhibitor with IC50 values of 11.73, 6.09 and 11.18 μM for PI3K-α、PI3K-β and PI3K-δ , respectively. PI3K-IN-33 arrests cell cycle at G2/M phase and induces apoptosis. PI3K-IN-33 can be used in leukemia research[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> PI3K/Akt/mTOR >> PI3K

PI3Kα:11.73 μM (IC50)

PI3Kβ:6.09 μM (IC50)

PI3Kδ:11.18 μM (IC50)

PI3K-IN-33 (Compound 6e) (10 μM, 48 hours) possess potent antiproliferative activity can inhibit proliferation of Leukemia SR cell lines in vitro[1]. PI3K-IN-33 (Compound 6e) induces cell cycle arrest toward the G2-M phase (30.3%) and leads to DNA synthesis and apoptosis[1]. PI3K-IN-33 (Compound 6e) (10 μM, 48 hours) results in apoptotic with 12.13% of cells in the early and latest age[1]. Cell Cytotoxicity Assay[1] Cell Line: Leukemia SR cell lines. Concentration: 10 μM Incubation Time: 48 hours Result: Antiproliferative activity with values of 0.76 μM.

[1]. Helwa AA, et al. Novel antiproliferative agents bearing morpholinopyrimidine scaffold as PI3K inhibitors and apoptosis inducers; design, synthesis and molecular docking. Bioorg Chem. 2020 Sep;102:104051.