PARP10-IN-1

PARP10-IN-1 is a PARP10 inhibitor with an IC₅₀ of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer^[1]. In Vitro:PARP10-IN-1 potently inhibits the catalytic domain of PARP10 with an IC₅₀ of 1.8 μM and exhibits 29-fold selectivity over full-length PARP11 in a cell-free MARylation assay^[1].
PARP10-IN-1 inhibits the catalytic domain of PARP10 with an IC₅₀ of 2.7 μM, exhibits >37-fold selectivity over all tested H-Y-E PARPs, >10-fold selectivity over most tested H-Y-Φ PARPs (PARP6, PARP8, PARP12, PARP11, PARP14, PARP15), 7-fold selectivity over PARP7, and 2.5-fold selectivity over PARP16_ΔTM in cell-free MARylation assays^[1].
PARP10-IN-1 (1-100 μM; 3 h) is membrane-permeable and inhibits PARP10 auto-MARylation (EC₅₀ = 11 μM) and PARP10-mediated MARylation of endogenous high molecular weight targets (EC₅₀ = 2.3 μM) in GFP-PARP10-transfected HEK293T cells^[1].