PARP1-IN-46 is a potent inhibitor of PARP-1 with an IC50 value of 2.4 nM. It demonstrates significant antiproliferative activity in both rat (C6) and human (U87MG) glioma cells. The compound triggers PARP cleavage, induces DNA damage, and elevates ROS levels. PARP1-IN-46 effectively impedes glioma cell migration, invasion, and colony formation, ultimately inducing apoptosis. It is suitable for research on glioma cells.

PARP1:2.4 nM

PARP1-IN-46 (Compound 5c) demonstrates consistent antiproliferative activity with IC50 values of 1.34 μM, 1.28 μM, 4.91 μM, and 1.37 μM against C6, U87MG, Ovcar-3, and A549 cells, respectively. It significantly inhibits migration, invasion, and colony formation in C6 and U87MG cells over 24 hours to 14 days. The compound also notably increases early and late apoptosis in C6 and U87MG cells within 24 hours. Furthermore, PARP1-IN-46 induces PARP protein cleavage, upregulates the DNA damage marker γ-H2AX, and downregulates the anti-apoptotic protein Bcl-2 in C6 cells. It leads to DNA damage and significantly raises ROS levels in C6 and U87MG cells.