Tankyrase-IN-2 is a selective, potent and orally active inhibitor of tankyrase with IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively

TNKS2:7 nM , PARP1:710 nM , TNKS1:10 nM

In DLD1 cells, Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance (EC50 of 320 nM). This is in the same potency range as the value for axin2 increase with EC50 of 319 nM.