compound introduction
Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor ( IC 50 s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1 , respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model In Vitro Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance with an EC 50 of 320 nM in DLD1 cells. This is in the same potency range as the value for axin2 increase (EC 50 =319 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)
