PARP11 inhibitor ITK7

PARP11 inhibitor ITK7 (ITK7) is a potent and selective PARP11 inhibitor. PARP11 inhibitor ITK7 can potently inhibit PARP11 with an IC50 value of 14 nM. PARP11 inhibitor ITK7 can be used for the research of cellular localization[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> PARP

Signaling Pathways >> Cell Cycle/DNA Damage >> PARP

IC50: 14 nM (PARP11); 13 nM (PARP11-dependent auto-MARylation)[1]

PARP11 inhibitor ITK7 (ITK7) 可有效抑制 PARP11，IC50 值为 14 nM[1]。 ITK7 对 PARP11 依赖性自体 MARylation 具有剂量依赖性抑制作用，EC50 值为 13 nM[1]。 ITK7 (0, 0.03, 0.1, 0.3, 1, 3 μM; 3 h) 抑制 PARP11 在细胞中的自甲基化活性，并导致 PARP11 从核膜分离[1]。 Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM Incubation Time: 3 h Result: Inhibited GFP-PARP11 auto-MARylation activity in a dose-dependent manner in HeLa cells.

[1]. Kirby, Ilsa T et al. A Potent and Selective PARP11 Inhibitor Suggests Coupling between Cellular Localization and Catalytic Activity. Cell chemical biology vol. 25,12 (2018): 1547-1553.e12.