UM-164: A c-Src/p38 Kinase Inhibitor inhibits proliferationand induces apoptosis in human glioblastoma cells

Abstract Glioblastoma is the most common and aggressive primary brain tumor in adults, which has high mortality and morbidity rates, and short survival time. here we tested a novel c-Src/p38 kinase inhibitor UM-164 in human glioblastoma cells in U87 and U251 cells. CCK-8 assay, EDU staining, colony formation, wound healing, cell cycle distribution analysis, migration and transwell invasion assays showed that UM-164 suppressed the proliferation and dose‑ and time‑dependent cytotoxicity in and exhibited a marked suppression after treating the U87 and U251 cells with UM-164. Flow cytometry, TUNNEL assays, immunofluorescent staining and western blotting test which tested the expression levels of BCL-2, BCL-XL, BAX, Cleaved-caspas-3, Cyclin D1, Cyclin E, MMP-2, MMP-9, P38, P-P38, EGFR, P-EGFR(Tyr1068), AKT, P-AKT, P42 and P-P42 were changed after um-164 treatment have changed and exhibited a strong inhibition for the proliferation and induces apoptosis. taken together, our findings indicate that um-164 exerts an antitumor effect by inhibiting proliferation and inducing apoptosis in human glioma cells. as for the present study provides evidence supportive of further development of multitarget kinase inhibitor UM-164 for adjuvant therapy and give a hope in GBM patients.