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Figure 1 | Journal of Hematology & Oncology

Figure 1

From: Identification of a promising PI3K inhibitor for the treatment of multiple myeloma through the structural optimization

Figure 1

BENC-511 displays potent inhibitory effects on AKT activation. (A) The structures of the analogs of S14161, including DQJ-610, DJY-611, WQD-612, QDF-510, BENC-511. (B) OPM2 cells were treated with 4 μM of S14161, BENC (BENC-511), QDF (QDF-510), DQJ (DQJ-610), DJY (DJY-611), or WQD (WQD-612) for 24 hours. After incubation, cells were harvested and total proteins were isolated. Expression of p-AKT (S473) and total AKT were measured by immunoblotting. (C) RPMI-8226 (8226), JJN3, OCI-MY5 (MY5), U266, LP1, OPM2 cells were treated with 4 μM of BENC-511 or DMSO for 24 hours followed by the analysis of the expression of p-AKT (S473) and total AKT. (D) RPMI-8226, LP1 and OPM2 cells were treated with increasing concentration of BENC-511 for 24 hours. Expression of p-AKT (S473 and T308), and total AKT were measured by immunoblotting. (E) RPMI-8226 and OPM2 cells were treated with increasing concentration of BENC-511 for 12 hours followed by the analysis of AKT activation. GAPDH was used as a loading control. T-AKT: total AKT.

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