PI3Kδ-IN-24 is a selective inhibitor of PI3Kδ with an IC50 value of 0.1 nM. It exhibits significant antiproliferative effects on cancer cell lines that overexpress PI3Kδ. PI3Kδ-IN-24 reduces p-AKT levels and induces cell cycle arrest and apoptosis in tumor cells. This compound is applicable for cancer research, particularly in diffuse large B-cell lymphoma (DLBCL).

PI3Kδ:0.1 nM

PI3Kδ-IN-24 (Compound M7) exerts inhibitory effects on the growth of SU-DHL-6 and Pfeiffer cells with GI50 values of 0.012 μM and 0.068 μM, respectively. It shows weaker antiproliferative activity against HCT-116, MCF-7, and Raji cells with GI50 values of 1.20 μM, 2.56 μM, and 6.83 μM, respectively. At concentrations ranging from 10-1000 nM over 24 hours, PI3Kδ-IN-24 consistently inhibits AKT phosphorylation in SU-DHL-6 cells. Additionally, a 0.5-hour treatment with 10 μM of PI3Kδ-IN-24 enhances the thermal stability of endogenous PI3Kδ in SU-DHL-6 cells. When administered at 0.01-1 μM for 24-72 hours, PI3Kδ-IN-24 induces cell cycle arrest in the G0/G1 phase and apoptosis in SU-DHL-6 cells, without causing apoptosis in HEK293 cells.